Month: October 2022

On August 21, 2015, Dong, Yi; Du, Nana; Li, Xueyuan; Zheng, Litao; Liu, Gang published an article.Category: alcohols-buliding-blocks The title of the article was Tandem Chloropalladation/Cyclization and Dearomative Cyclization toward Functionalized Tricyclic Bridged [3.2.1] Skeleton Compounds. And the article contained the following:

In the presence of PdCl2(MeCN)2 and CuCl2, o-alkenylphenylalkynyl carbonyl compounds such as allyloxyphenylpropynamide I underwent aerobic chemoselective dearomative cyclization reactions to yield fused tricyclic dienones such as II (R = MeO, BuO, EtO, PhCH2O, Me). The structure of II (R = PhCH2O) was determined by X-ray crystallog. The experimental process involved the reaction of 2,4,6-Trihydroxy-3-methylbenzaldehyde(cas: 55743-13-0).Category: alcohols-buliding-blocks

The Article related to fused tricyclic dienone chemoselective preparation, palladium copper catalyst aerobic dearomative cyclization alkenylphenylalkynyl carbonyl compound, tandem aerobic chloropalladation dearomative cyclization alkenylphenylalkynyl carbonyl compound, oxatricyclododecanecarboxamide mol crystal structure and other aspects.Category: alcohols-buliding-blocks

Referemce:
Alcohol – Wikipedia,
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On November 30, 2012, Sinha, Debarshi; Mandal, Tanmay; Gogoi, Sanjib; Goldman, Joshua J.; Zhao, John Cong-gui published an article.Recommanded Product: H-Phg(4-OH)-OH The title of the article was Asymmetric Aldol Reaction Catalyzed by Modularly Designed Organocatalysts. And the article contained the following:

The self-assembly of pre-catalyst modules, which are amino acids and cinchona alkaloid derivatives, leads to a direct formation of the desired organocatalysts without any synthesis. These modularly designed organocatalysts (MDOs) may be used for catalyzed asym. aldol reaction. Depending on structure of the aldehyde substrates, the corresponding aldol products may be obtained in mediocre to excellent enantiomeric excess (ee) values (up to 92% ee) with moderate diastereoselectivities (up to 79:21 diastereomeric ratio, dr). The synthesis of the target compounds was achieved by a combination of amino acids and analogs, such as (αS)-α-amino-2-chlorobenzeneacetic acid, L-alanine, L-leucine, L-isoleucine. 3-methyl-L-valine, β-alanine. Cinchona alkaloids included N-[3,5-bis(trifluoromethyl)phenyl]-N’-[(8α,9S)-6′-methoxycinchonan-9-yl]thiourea, (8α,9R)-cinchonan-6′,9-diol (cupreine), (9S)-cinchonan-6′,9-diol (cupreidine), O-benzoylquinine, (8α,9R)-6′-methoxy-9-(phenylmethoxy)cinchonan (O-benzylquinine), etc. The title compounds thus formed included (4S)-4-hydroxy-4-(4-nitrophenyl)-2-butanone (4R)-4-hydroxy-4-(4-nitrophenyl)-2-butanone and (2R)-2-[(R)-hydroxy(4-nitrophenyl)methyl]cyclohexanone (I) and related substances, such as (3R)-tetrahydro-3-[(R)-hydroxy(4-nitrophenyl)methyl]-4H-pyran-4-one, (3R)-tetrahydro-3-[(R)-hydroxy(4-nitrophenyl)methyl]-4H-thiopyran-4-one. The experimental process involved the reaction of H-Phg(4-OH)-OH(cas: 32462-30-9).Recommanded Product: H-Phg(4-OH)-OH

The Article related to cinchona alkaloid amino acid chiral catalyst aldol reaction, cyclohexanone hydroxyalkyl preparation aldol addition cinchona alkaloid catalyst, pyranone hydroxyalkyl preparation aldol addition cinchona alkaloid catalyst, thiopyranone hydroxyalkyl preparation aldol addition cinchona alkaloid catalyst and other aspects.Recommanded Product: H-Phg(4-OH)-OH

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Alcohol – Wikipedia,
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On April 16, 2021, Sunagawa, Denise E.; Ishida, Naoyoshi; Iwamoto, Hiroaki; Ohashi, Masato; Fruit, Corinne; Ogoshi, Sensuke published an article.HPLC of Formula: 143-10-2 The title of the article was Synthesis of Fluoroalkyl Sulfides via Additive-Free Hydrothiolation and Sequential Functionalization Reactions. And the article contained the following:

A modular synthetic method, involving a hydrothiolation, silylation, and fluoroalkylation, for the construction of highly functionalized fluoroalkyl sulfides has been developed. The use of the aprotic polar solvent N,N-dimethylacetamide enables the additive-free chemoselective hydrothiolation of tetrafluoroethylene, trifluorochloroethylene, and hexafluoropropene with various thiols. Stepwise functionalization of the tetrafluoroethyl ethers and a chlorotrifluoroethyl ether by silylation with TMSCl and LDA followed by reactions with aryl iodides, a chloroalkene, or acyl chlorides in the presence of CuOt-Bu and 1,10-phenanthroline convert the hydrothiolated intermediates into the tetrafluoroethyl sulfides in high efficiency. The method avoids the use of the environmental pollutant Halon-2402 (1,2-dibromo-1,1,2,2-tetrafluoroethane), which was employed as a building block in a reported synthetic route. Tetrafluoroethylene is a potential carcinogen and should be used in a well-ventilated fume hood. The experimental process involved the reaction of 1-Decanethiol(cas: 143-10-2).HPLC of Formula: 143-10-2

The Article related to tetrafluoroethyl silyltetrafluoroethyl thioether chemoselective preparation, dimethylacetamide solvent hydrothiolation tetrafluoroethylene chlorotrifluoroethylene hexafluoropropene thiol, fluoroalkyl thioether modular preparation, base mediated silylation hydrofluoroalkyl thioether chlorotrimethylsilane and other aspects.HPLC of Formula: 143-10-2

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Alcohol – Wikipedia,
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On January 11, 2021, Talukder, Muktadir Md; Miller, Justin T.; Cue, John Michael O.; Udamulle, Chinthaka M.; Bhadran, Abhi; Biewer, Michael C.; Stefan, Mihaela C. published an article.Application In Synthesis of 1-Decanethiol The title of the article was Mono- and Dinuclear α-Diimine Nickel(II) and Palladium(II) Complexes in C-S Cross-Coupling. And the article contained the following:

The usefulness of transition metal catalytic systems in C-S cross-coupling reactions is significantly reduced by air and moisture sensitivity, as well as harsh reaction conditions. Herein, the authors report four highly air- and moisture-stable well-defined mononuclear and bridged dinuclear α-diimine Ni(II) and Pd(II) complexes for C-S cross-coupling. Various ligand frameworks, including acenaphthene- and iminopyridine-based ligands, were employed, and the resulting steric properties of the catalysts were evaluated and correlated with reaction outcomes. Under aerobic conditions and low temperatures, both Ni and Pd systems exhibited broader substrate scope and functional group tolerance than previously reported catalysts. Over 40 compounds were synthesized from thiols containing alkyl, benzyl, and heteroaryl groups. Also, pharmaceutically active heteroaryl moieties are incorporated from thiol and halide sources. Notably, the bridged dinuclear five-coordinate Ni complex has outperformed the remaining three mono four- or six-coordinate complexes by giving almost quant. yields across a broad substrate scope. The experimental process involved the reaction of 1-Decanethiol(cas: 143-10-2).Application In Synthesis of 1-Decanethiol

The Article related to mononuclear diimine palladium complex preparation catalyst thiol coupling reaction, crystal structure mononuclear dinuclear diimine nickel palladium complex, mol structure mononuclear dinuclear diimine nickel palladium complex, dinuclear diimine nickel complex preparation catalyst thiol coupling reaction and other aspects.Application In Synthesis of 1-Decanethiol

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Alcohol – Wikipedia,
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On June 21, 2003, Kuehne, Martin E.; Bornmann, William G.; Marko, Istvan; Qin, Yong; LeBoulluec, Karen L.; Frasier, Deborah A.; Xu, Feng; Mulamba, Tshilundu; Ensinger, Carol L.; Borman, Linda S.; Huot, Anne E.; Exon, Christopher; Bizzarro, Fred T.; Cheung, Julia B.; Bane, Susan L. published an article.Related Products of 42900-89-0 The title of the article was Syntheses and biological evaluation of vinblastine congeners. And the article contained the following:

Sixty-two congeners of vinblastine (VLB), e.g. I, , primarily with modifications of the piperidine ring in the carbomethoxycleavamine moiety of the binary alkaloid, were synthesized. For example, I was prepared starting from δ-valerolactone (II). Methylation of II at the 3-position followed by ring opening gave MeO2CCH(Me)CH2CH2CHO which was reacted with indoloazepine III. The resulting bridged indoloazepine was N-benzylated to give pyrrolocarbazolecarboxylate IV. IV then went through a series of reactions, including addition to vindoline to give I in 81% yield. These compounds were evaluated for cytotoxicity against murine L1210 leukemia and RCC-2 rat colon cancer cells, and for their ability to inhibit polymerization of microtubular protein at <10-6 M, and for induction of spiralization of microtubular protein, and for microtubular disassembly at 10-4 M concentrations An ID50 range of >107 M concentrations was found for L1210 inhibition by these compounds, with the most active 1000× as potent as vinblastine. The experimental process involved the reaction of Isochroman-3-ol(cas: 42900-89-0).Related Products of 42900-89-0

The Article related to vinblastine congener preparation antitumor, microtubular disassembly spiralization induction polymerization inhibition vinblastine congener, spiralization induction microtubular vinblastine congener, polymerization inhibition microtubular vinblastine congener, colon adenocarcinoma inhibition vinblastine congener and other aspects.Related Products of 42900-89-0

Referemce:
Alcohol – Wikipedia,
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On May 28, 2020, Zhong, Wenge published a patent.Category: alcohols-buliding-blocks The title of the patent was Preparation of 1H-benzimidazole-6-carboxylic acid derivatives as glucagon-like peptide-1 receptor (GLP-1R) agonists and uses thereof. And the patent contained the following:

The title compounds represented by formula I (X1-X5, Y1-Y5, Z1-Z4, T2-T4, T6-T8, Ra, Rb, Rc, Rd, R1-R3, m, n, and o are defined below) or pharmaceutically acceptable salts, stereoisomers, solvates, or hydrates thereof are prepared for use in, e.g. treating type 2 diabetes mellitus, pre-diabetes, obesity, non-alc. fatty liver disease, non-alc. steatohepatitis, and cardiovascular disease. X1-X5, Y1-Y5, Z1-Z4, T2-T4, and T6-T8 are defined as [the dashed line with a solid line = a single bond or a double bond; X1, X2, X3, X4, X5 = each independently N or CH, wherein no more than three of X1-X5 are N and ring A does not contain 3-nitrogen ring atoms at 3 contiguous positions; W = O, S, or each (un)substituted CH2 or NH; Y1, Y3, Y4, Y5 = each independently N, NH, CH, or CH2; Y2, Y6 = each independently N, C, or CH, wherein there is no more than 3-nitrogen ring atoms in ring B and ring B does not contain 3-nitrogen ring atoms at 3 contiguous positions; Z1, Z2 = each independently N, C, or CH, wherein at least one of Z1 and Z2 is N; Z3, Z4 = each independently a bond, CH, CH2, CH:CH, CH2CH2, CH2CH, or CHCH2, wherein ring C contains no more than two double bonds; provided that when ring B = (un)substituted pyridine-2,6-diyl, then (1) W is not O, and/or (2) ring C is not (un)substituted piperazine-1,4-diyl and/or (3) ring C is not (un)substituted piperidine-1,4-diyl; wherein Z1 is N, and/or (4) ring A is not phenyl; T2, T3, T4 = each independently N, O, S, C, or each (un)substituted NH or CH ; T6, T6, T8 = each independently selected N or (un)substituted CH; wherein no more than 4 of T2, T3, T4, T6, T7, and T8 are selected from N, O, and S; EE = CO2H or a carboxylic group surrogate (e.g. C(O)CF3, CH(F)CF3, C(O)NHCN, C(O)NHOH, C(O)NHOMe, 2H-tetrazol-2-yl, etc.)]. Ra, Rb, Rc, and Rd are defined as [Ra = hydrogen, deuterium, halogen, cyano, or each (un)substituted C1-6 alkyl, C1-6 alkoxy, NH2, 6-10 membered aryl, 5-8 membered heteroaryl, 3-8 membered saturated or partially saturated cycloalkyl, 3-8 membered saturated or partially saturated heterocyclyl; Rb = hydrogen, deuterium, halogen, cyano, or each (un)substituted C1-6 alkyl, C1-6 alkoxy, NH2, 6-10 membered aryl, 5-8 membered heteroaryl, 3-8 membered saturated or partially saturated cycloalkyl, or 3-8 membered saturated or partially saturated heterocyclyl; Rc = hydrogen, deuterium, halogen, cyano, or each (un)substituted C1-6 alkyl, C1-6 alkoxy, NH2, 6-10 membered aryl, 5-8 membered heteroaryl, 3-8 membered saturated or partially saturated cycloalkyl, or 3-8 membered saturated or partially saturated heterocyclyl; Rd = hydrogen, deuterium, halogen, cyano, or each (un)substituted C1-6 alkyl, C1-6 alkoxy, NH2, 6-10 membered aryl, 5-8 membered heteroaryl, 3-8 membered saturated or partially saturated cycloalkyl, or 3-8 membered saturated or partially saturated heterocyclyl]. R1-R3, m, n, and o are defined as [R1 = independently halogen, cyano, OH, or each (un)substituted C1-6 alkyl, C1-6 alkoxy, C2-6 alkenyl, C2-6 alkynyl, NH2, 6-10 membered aryl, 5-8 membered heteroaryl, 3-8 membered saturated or partially saturated cycloalkyl, or 3-8 membered saturated or partially saturated heterocyclyl; R2 = independently halogen, cyano, OH, oxo, or each (un)substituted C1-6 alkyl, C1-6 alkoxy, NH2, 6-10 membered aryl, 5-8 membered heteroaryl, 3-8 membered saturated or partially saturated cycloalkyl, or 3-8 membered saturated or partially saturated heterocyclyl; R3 = independently halogen, cyano, OH, oxo, or each (un)substituted C1-6 alkyl, C1-6 alkoxy, NH2, 6-10 membered aryl, 5-8 membered heteroaryl, 3-8 membered saturated or partially saturated cycloalkyl, or 3-8 membered saturated or partially saturated heterocyclyl; m = an integer of 0-4; n, o = each independently an integer of 0-5]. Thus, sequential amination of 2,6-dichloropyridine with tert-Bu piperazine-1-carboxylate in DMSO at 110° for 12 h and (4-chloro-2-fluorophenyl)methanamine in the presence of BINAP, Pd2(dba)2, sodium tert-butoxide in toluene at 100° for 12 h gave tert-Bu 4-[6-(4-chloro-2-fluorobenzylamino)pyridin-2-yl]piperazine-1-carboxylate which was treated with CF3CO2H in CH2Cl2 and underwent alkylation with tert-Bu (S)-2-(chloromethyl)-1-(oxetan-2-ylmethyl)-1H-benzimidazole-6-carboxylate in the presence of K2CO3 in DMF at 90° for 5 h and deprotection by treatment with CF3CO2H to give (S)-2-[[4-[6-(4-chloro-2-fluorobenzylamino)pyridin-2-yl]piperazin-1-yl]methyl]-1-(oxetan-2-ylmethyl)-1H-benzimidazole-6-carboxylic acid (II). II in vitro showed EC50 of ≤0.015μM for production of cAMP in HEK293T cells expressing human GLP-1R. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Category: alcohols-buliding-blocks

The Article related to benzimidazolecarboxylic acid preparation glp 1r agonist, oxetanylmethylbenzimidazolecarboxylic acid preparation glp 1r agonist, piperazinylmethyloxetanylmethylbenzimidazolecarboxylic acid preparation glp 1r agonist, glucagon peptide 1 receptor glp 1r agonist, type 2 diabetes mellitus prediabetes obesity treatment and other aspects.Category: alcohols-buliding-blocks

Referemce:
Alcohol – Wikipedia,
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On February 15, 2020, Paudel, Kushal; Hauk, Armin; Maier, Tanja Verena; Menzel, Roberto published an article.Related Products of 96-76-4 The title of the article was Quantitative characterization of leachables sinks in biopharmaceutical downstream processing. And the article contained the following:

This article demonstrates, on a quant. level, that leachables – potentially accumulated during a biopharmaceutical manufacturing process – will be significantly reduced/removed during four key downstream process steps: cell removal using centrifugation or depth filtration, sterile filtration and virus filtration. Eight common leachables model compounds (LMCs) were spiked into typical feed solutions containing buffer and proteins and were analyzed post-processing in the supernatant or filtrates by HPLC-UV. The clearance rates were calculated as the quotient between the scavenged and initially spiked amount of each leachable. High clearance rates were found for hydrophobic LMCs for all investigated downstream operation steps. It is shown that the removal of cells and cell debris from a culture broth reduces the amount of LMCs almost completely after centrifugation or depth filtration. Also, sterilizing-grade and virus filtration provided a high scavenger effect to most of the LMCs. In contrast, only one hydrophilic acid was not significantly scavenged by the described operations. The possibility to include leachables sinks to a process qualification and risk mitigation concept is explained. The experimental process involved the reaction of 2,4-Di-tert-butylphenol(cas: 96-76-4).Related Products of 96-76-4

The Article related to biopharmaceutical downstream processing leachable depth sterile virus filtration, biopharmaceutical manufacturing, cell removal, downstream processing, extractables and leachables, leachables sink, process equipment-related leachables (perls), single-use system (sus), sterilizing-grade filtration, virus filtration and other aspects.Related Products of 96-76-4

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Alcohol – Wikipedia,
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On June 19, 1990, Kuehne, Martin published a patent.Safety of Isochroman-3-ol The title of the patent was Preparation of cycloalkyl and aromatic moieties-containing vinblastines and vincristines as antitumors. And the patent contained the following:

The title compounds [I; R1R2 = alkylene, benzo; R10 = HCO, Me; R11 = alkoxy, trialkylammoniumyl; R12 = alkanoyloxy, OH; R13 = alkyl] were prepared Vindoline-HCl was condensed with Me (3aRS,4RS,11bSR)]-3-benzyl-4-[2-(tert-butyldimethylsilyloxymethyl)phenyl]-1,2,3,3a,4,5-hexahydro-7H-pyrrolo[2,3-d]carbazole-6-carboxylate to give, after desilylation, a 1:1 mixture of (5R,7S)-3-benzyl-5-[2-(hydroxymethyl)phenyl]-1,2,3,4,5,6,7,8-octahydroazonino[5,4-b]indole-7-(15-vindolinyl)-7-carboxylate (II) and its 5R,7R-diastereomer. II was then cyclized in CH2Cl2 containing Et3N and p-toluenesulfonic anhydride to give, after hydrogenolysis, (9R,11S)-15-[1,2,4,9,10,11,12,17-octahydro-11-(methoxycarbonyl)indolo[2′,3′:6,7]azonino[1,2,3:bc]isoquinolin-11-yl]vindoline (III). III had an ED50 comparable to that of vinblastine against P388 leukemia cells resistant to adriamycin. The experimental process involved the reaction of Isochroman-3-ol(cas: 42900-89-0).Safety of Isochroman-3-ol

The Article related to vinblastine cycloalkyl aryl preparation antitumor, cycloalkylvinblastine preparation antitumor, vincristine cycloalkyl aryl preparation antitumor, cycloalkylvincristine preparation antitumor, antitumor vinblastine vincristine cycloalkyl aryl, arylvinblastine preparation antitumor, arylvincristine preparation antitumor and other aspects.Safety of Isochroman-3-ol

Referemce:
Alcohol – Wikipedia,
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Flinker, Mathias; Yin, Hongfei; Juhl, Rene W.; Eikeland, Espen Z.; Overgaard, Jacob; Nielsen, Dennis U.; Skrydstrup, Troels published an article in 2017, the title of the article was Efficient Water Reduction with sp3-sp3 Diboron(4) Compounds: Application to Hydrogenations, H-D Exchange Reactions, and Carbonyl Reductions.Recommanded Product: 2160-93-2 And the article contains the following content:

Diboron complexes with aminodiols and aminotriols such as I were prepared or generated in situ from (HO)2BB(OH)2; the diboron compounds reduced H2O or D2O to yield H2 or D2 which was used for chemoselective alkene and stereoselective diaryl alkyne hydrogenation, deuterium exchanges, and aldehyde and ketone reductions to alcs. in a two-chamber reactor. The experimental process involved the reaction of 2,2′-(tert-Butylazanediyl)diethanol(cas: 2160-93-2).Recommanded Product: 2160-93-2

The Article related to chemoselective hydrogenation deuterium exchange carbonyl reduction diboron diethanolamine complex, diboron aminodiol aminotriol complex preparation reductant hydrogen generation, reduction water hydrogen diboron aminodiol aminotriol complex reductant, alkene alkyne chemoselective hydrogenation water hydrogen source diboron and other aspects.Recommanded Product: 2160-93-2

Referemce:
Alcohol – Wikipedia,
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On March 5, 2022, Fang, Yuying; Tan, Qingyun; Zhou, Huihao; Gu, Qiong; Xu, Jun published an article.Application In Synthesis of 3-Hydroxyphenylacetic acid The title of the article was Discovery of novel diphenylbutene derivative ferroptosis inhibitors as neuroprotective agents. And the article contained the following:

Herein, with phenotypic assays, a new diphenylbutene derivative ferroptosis inhibitor, DPT was discovered. Based on this hit, new diphenylbutene derivatives I [R1 = H, 2-OMe, 3-OH, etc.; R2 = H, 3-OH, 4-OH, etc.] synthesized via condensation of (piperazinyl)pyrimidine and (phenyl)-phenylpentadienoic acids II and evaluated their ferroptosis inhibitory activities in HT22 mouse hippocampal neuronal cells and found that three compounds exhibited improved inhibitory activities compared with DPT. Among these active compounds, compound I [R1 = 3-OMe-4-HOC6H4, R2 = H] displayed the most potent anti-ferroptosis activity (EC50 = 1.7μM). Further studies demonstrated that compound I [R1 = 3-OMe-4-HOC6H4, R2 = H] was a specific ferroptosis inhibitor. It was revealed that different than the classic ferroptosis inhibitors, compound I [R1 = 3-OMe-4-HOC6H4, R2 = H] blocked ferroptosis by increasing FSP1 protein level. Compound I [R1 = 3-OMe-4-HOC6H4, R2 = H] could penetrate blood-brain barrier (BBB). In a rat model of ischemic stroke, compound I [R1 = 3-OMe-4-HOC6H4, R2 = H] effectively mitigated cerebral ischemic injury. Therefore, it was confirmed that compound I [R1 = 3-OMe-4-HOC6H4, R2 = H] as a novel ferroptosis inhibitor with a new scaffold, was promising for further development as an agent against neurol. diseases. The experimental process involved the reaction of 3-Hydroxyphenylacetic acid(cas: 621-37-4).Application In Synthesis of 3-Hydroxyphenylacetic acid

The Article related to phenyl pyrimidinyl piperazinyl pentadienone diastereoselective preparation ferroptosis inhibitor dpt, piperazinyl pentadienone phenyl pyrimidinyl diastereoselective preparation adme human, phenylpentadienoic phenyl acid preparation piperazinyl pyrimidine condensation, cinnamaldehyde phenylacetic acid perkin, diphenylbutene, fsp1 and other aspects.Application In Synthesis of 3-Hydroxyphenylacetic acid

Referemce:
Alcohol – Wikipedia,
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