Tag: 100-200

On August 31, 2019, Sekerova, Lada; Spacilova, Marketa; Vyskocilova, Eliska; Krupka, Jiri; Cerveny, Libor published an article.Computed Properties of 78-26-2 The title of the article was Acid catalyzed acetalization of aldehydes with diols resulting into the formation of fragrant cyclic acetals. And the article contained the following:

The influence of reaction conditions (amount and type of the catalyst, the reaction temperature, the type of the solvent) on the reaction course of the acetalization of aldehydes with diols was tested in this paper. The optimization of reaction conditions was performed on model reaction, acetalization of 2-methylpentanal by 2-methyl-2-propyl-1,3-propanediol leading to the formation of fragrant compound 2-(1-methylbutyl)-5-methyl-5-propyl-1,3-dioxane (Troenan). Para toluenesulfonic acid was used as an active homogeneous catalyst. It appeared to be advantageous not to use any solvent in the reaction. Using 0.3 wt% of the catalyst the almost total conversion of 2-methylpentanal was achieved after 240 min of reaction at room temperature while the selectivity to the desired product was about 98%. The optimized reaction conditions were applied to the preparation of four cyclic fragrant acetals (namely 2-hexyl-1,3-dioxolane, 2-hexyl-4-methyl-1,3-dioxolane, 2-benzyl-5-hydroxy-1,3-dioxane and 2-(1-methylbutyl)-5-methyl-5-propyl-1,3-dioxane) in larger scale; and these were sensory evaluated after purification step. Prepared heterogeneous catalysts, acid modified montmorillonite (MMT) K-10 (treated by H2SO4, HNO3, and HCl) were successful in the model reaction. The conversion of 2-methylpentanal over 90% was achieved using acid modified MMT after 300 min of reaction at room temperature, the selectivity to the desired product was about 98%. MMT/H2SO4 can be used in the model reaction four times without any change in the reaction course, what makes it promising for the further application. The experimental process involved the reaction of 2-Methyl-2-propylpropane-1,3-diol(cas: 78-26-2).Computed Properties of 78-26-2

The Article related to fragrant cyclic acetal preparation aldehyde diol acid catalysis, Industrial Organic Chemicals, Leather, Fats, and Waxes: Manufacture Of Industrial Organic Chemicals and other aspects.Computed Properties of 78-26-2

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On October 24, 2019, Lauffer, David J.; Bemis, Guy; Boyd, Michael; Deininger, David; Deng, Hongbo; Dorsch, Warren; Gu, Wenxin; Hoover, Russell R.; Johnson, Jr., Mac Arthur; Ledeboer, Mark Willem; Ledford, Brian; Maltais, Francois; Penney, Marina; Takemoto, Darin; Waal, Nathan D.; Weng, Tiansheng published a patent.Application of 386704-04-7 The title of the patent was Preparation of pteridinone compounds for the treatment of cellular proliferative disorders. And the patent contained the following:

The invention provides compounds of formula I, or pharmaceutically acceptable salts thereof, pharmaceutical compositions thereof, and methods of use thereof for treating cellular proliferative disorders (e.g., cancer). Compounds of formula I wherein A is (un)saturated 3- to 8-membered carbocyclic ring, indanyl, Ph, (un)saturated 4- to 8-membered monocyclic heterocyclic ring; L is a bond, (un)branched C1-6 hydrocarbyl and (un)branched C1-6 heterohydrocarbyl; R1 is H, (un)substituted C1-4 aliphatic, R’, etc.; R2 and R2′ are independently H, R’, (un)substituted C1-4 aliphatic, etc.; R3 is H, R’, and (un)substituted C1-6 aliphatic; R4 is H, R’, CH2OH, etc.; R5 is H, acyl, CO2H and derivatives, etc.;each R6 is independently halo, CN, NO2, acyl, etc.; R’ is C1-4 deuterioaliph.; X is N and CH; n is 0, 1, 2, 3, 4 and 5; and pharmaceutically acceptable salts thereof, are claimed. Example compound II was prepared by a general procedure (procedure given). The invention compounds were evaluated for their PLK1 inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value of < 0.3 μM. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Application of 386704-04-7

The Article related to pteridinone preparation treatment cellular proliferative disorder, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Application of 386704-04-7

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On December 11, 2008, Bernasconi, Giovanni; Bromidge, Steven Mark; Carpenter, Andrew James; D’Adamo, Lucilla; Di Fabio, Romano; Guery, Sebastien; Pavone, Francesca; Pozzan, Alfonso; Rinaldi, Marilisa; Sabbatini, Fabio Maria; St-Denis, Yves published a patent.SDS of cas: 386704-04-7 The title of the patent was Preparation of N-phenyl piperidinyl- and piperazinylacetohydrazides as modulators of the ghrelin receptor. And the patent contained the following:

Title compounds [I; R1 = Cl, Br, Me, CF3; X = C, N; R1a = H, alkyl; R2a = H, Me; R2 = alkyl, H, (CH2)n, wherein n = 3, 4 and the terminal C of the chain is bonded to the C atom adjacent to the N bearing the R2 group, such that a fused 6,5 or 6,6-bicyclic ring is formed; Y = (substituted) Ph pyridyl, naphthyl, pyrimidinyl, imidazo[1,2-a]pyridine-6-yl, benzothiophen-2-yl, benzothiophen-5-yl, benzofuran-2-yl, dibenzo[b,d]furan-3-yl, dibenzo[b,d]thiophen-2-yl, dibenzo[b,d]thiophen-4-yl, 1,3-benzodioxol-5-yl, 2,3-dihydro-1,4-benzodioxin-5-yl, 2,3-dihydro-1,4-benzodioxin-6-yl, 2,3-dihydro-1-benzofuran-4-yl, 2,2-difluoro-1,3-benzodiox-4-yl, pyridazinyl, imidazolyl, oxazolyl, pyrazolyl, thiazolyl, triazolyl; when Y = 2,3-dihydro-1,4-benzodioxin-6-yl, R1 ≠ Cl], were prepared Thus, dibenzo[b,d]thien-4-ylboronic acid, glyoxylic acid hydrate, and 1-methylpiperazine were microwaved together in MeCN at 120° for 20 min. to give 53% dibenzo[b,d]thien-4-yl(4-methyl-1-piperazinyl)acetic acid hydrochloride. This was stirred with TBTU, PL-DIPAM, and 3,5-dichlorophenylhydrazine in DMF for 24 h at room temperature to give 31% 2-dibenzo[b,d]thien-4-yl-N’-(3,5-dichlorophenyl)-2-(4-methyl-1-piperazinyl)acetohydrazide formate. The latter and other I showed pIC50 values of >5.5 in the GHSR antagonist BACMAM FLIPR assay. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).SDS of cas: 386704-04-7

The Article related to piperazinylacetohydrazide preparation ghrelin receptor modulator, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.SDS of cas: 386704-04-7

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On February 11, 2016, Claremon, David A.; Dong, Chengguo; Fan, Yi; Leftheris, Katerina; Lotesta, Stephen D.; Singh, Suresh B.; Tice, Colin M.; Zhao, Wei; Zheng, Yajun; Zhuang, Linghang published a patent.Application of 386704-04-7 The title of the patent was Preparation of piperazine derivatives as liver X receptor modulators. And the patent contained the following:

Provided are novel compounds of formula I, pharmaceutically acceptable salts thereof, and pharmaceutical compositions thereof, which are liver X receptor modulators, and which are useful in the treatment of diseases and disorders associated with the liver X receptor. Also provided are the compounds of formula I and pharmaceutical compositions thereof for treating atherosclerosis, cardiovascular disease, Alzheimer’s disease, dermatitis, dyslipidemia, cancer and other diseases or disorders. Title compounds I [Q = alkyl-OC(O), heteroaryl, aryl-alkyl-OC(O), etc.; R1 = alkyl, cycloalkyl, aryl-alkyl, etc.; R2 = H, halo, cyano, etc.; R3 = alkyl, halo-alkyl, cycloalkyl, etc.; R4 = H or alkyl], and their pharmaceutically acceptable salts, are prepared Thus, e.g., II was prepared by reaction of (R)-tert-Bu 2-isopropylpiperazine-1-carboxylate with [3-(methylsulfonyl)phenyl]boronic acid. Compounds of the invention were evaluated for their LXr α/β binding ad agonist activity, e.g., II showed Ki value of 1690 nM and 157 nM on LXRα and LXRβ, resp. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).Application of 386704-04-7

The Article related to piperazine derivative preparation liver receptor lxr modulator, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Application of 386704-04-7

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On March 30, 2021, Guo, Hongli; Chen, Tao; Zhou, Feng; Gao, Daxin; Chen, Dawei published a patent.Reference of (R)-(4-Methylmorpholin-3-yl)methanol The title of the patent was Preparation of quinazoline-based compounds as KRAS G12C inhibitor for treatment and/or alleviation of KRAS G12C-related diseases. And the patent contained the following:

The present invention relates to preparation of quinazoline-based compounds as KRAS G12C inhibitor for treatment and/or alleviation of KRAS G12C-related diseases. In particular, the quinazoline-based compound I (wherein, α and β bonds are single bonds or double bonds, resp.; X = N or CR2; when the β bond is a single bond, Y = C(O) and Z = NR3; when the β bond is a double bond, Y and Z are independently N or CR2; when the α bond is a single bond, W = N and V = CH2 or C(O); when the a bond is a double bond, W = C and V = CR4 or N; U and M are each independently N, C or CH; ring A = Ph, 3-8 membered cycloalkyl, 5-6 membered heteroaryl or 4-8 membered heterocycloalkyl group; the A ring is unsubstituted or optionally substituted). Further, (ring B = 5-10 membered heterocycloalkyl; the B ring is unsubstituted or optionally substituted; R = C6-10 aryl, 5-10 membered heteroaryl or 9-14 membered fused heterocycloalkyl group; said R is unsubstituted or optionally substituted; R1 = C2-4 alkenyl, C2-4 alkynyl or partially unsaturated C4-6 cycloalkyl; said R1 is unsubstituted or optionally substituted; R2 = H, hydroxyl, halogen, cyano, amino etc.; R3 = C3-8 cycloalkyl, 3-8 membered heterocycloalkyl, C6-10 aryl, 5-10 heteroaryl, C3-8 cycloalkyl-C1-4 alkyl etc.; R4 = H, hydroxyl, halogen, C2-6 alkenyl, C2-6 alkynyl, cyano, amino etc.), its isomers, stable isotope derivatives or pharmaceutically acceptable salts were prepared The inventive compound and its composition disclosed can effectively treat diseases related to KRAS G12C, such as cancer. The experimental process involved the reaction of (R)-(4-Methylmorpholin-3-yl)methanol(cas: 1620510-51-1).Reference of (R)-(4-Methylmorpholin-3-yl)methanol

The Article related to quinazoline compound preparation kras g12c inhibitor antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Reference of (R)-(4-Methylmorpholin-3-yl)methanol

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On November 29, 2018, Li, Liansheng; Feng, Jun; Wu, Tao; Liu, Yuan; Wang, Yi; Ren, Pingda; Liu, Yi published a patent.SDS of cas: 1620510-51-1 The title of the patent was Preparation of substituted quinazolines as covalent inhibitors of KRAS. And the patent contained the following:

The title compounds I [G1 and G2 = (independently) N or CH; L1 = a bond or NR6; L2 = a bond or alkylene; L3 = a bond, O, NR6, S, S(O) or SO2; R1 = unsubstituted naphthyl or optionally substituted quinolinyl when at least one of R31, R32, R41 and R42 is not H; or R1 = II (A1-A4 = (independently) C or N; X = O, S, N, etc.;Y = O, S, N, etc.; Z = O, S, N, etc.; one of R11-R14 is a covalent bond to the carbon attached to R1, and the other of R11-R14 = (independently) H, NH2, CN, etc.; R21-R23 = (independently) H, NH2, CN, etc.; R31 and R32 = (independently) H, OH, NH2, etc.; R41 and R42 = (independently) H, OH, NH2, etc.; R5 = NH2, CN, OH, etc.; R6 = (independently) H or alkyl; m and n = (independently) 1-3; and E = an electrophilic moiety capable of forming a covalent bond with the cysteine residue at position 12 of a KRAS, HRAS or NRAS G12C mutant protein)] or pharmaceutically acceptable salts, isotopic forms, stereoisomers or prodrugs thereof, having activity as inhibitors of G12C mutant KRAS protein, were prepared E.g., a multi-step synthesis of (2R,5S)-III, starting from 2-amino-4-bromo-3-fluorobenzoic acid, was described. Representative compounds I were tested and found to covalently bind to (or modify) KRAS G12C after a ten minute incubation period (data given). Pharmaceutical compositions comprising compounds I, and methods to modulate the activity of G12C mutant KRAS protein for treatment of disorders, such as cancer, were also provided. The experimental process involved the reaction of (R)-(4-Methylmorpholin-3-yl)methanol(cas: 1620510-51-1).SDS of cas: 1620510-51-1

The Article related to quinazoline preparation g12c mutant kras inhibitor antitumor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.SDS of cas: 1620510-51-1

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On July 11, 2019, Qian, Wenyuan; Yang, Chundao; Xu, Guanghai; Li, Jie; Li, Jian; Chen, Shuhui published a patent.SDS of cas: 386704-04-7 The title of the patent was Preparation of isoindolinone and derivatives thereof as CSF-1R inhibitors. And the patent contained the following:

The present invention relates to a type of isoindolinone derivatives and use thereof in the preparation of a medicament for treating diseases associated with a novel colony stimulating factor 1 receptor (CSF-1R) inhibitor. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).SDS of cas: 386704-04-7

The Article related to isoindolinone preparation colony stimulating factor receptor, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.SDS of cas: 386704-04-7

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On December 25, 2007, Xu, Hao; Han, Guozhi; Sha, Fei; Xu, Jian; Yao, Cheng published an article.Application of 2160-93-2 The title of the article was Synthesis of N-(tert-butyl)piperazine. And the article contained the following:

A method for the synthesis of the title compound is reported here. The synthetic sequence involved a condensation of tert-butylamine (i.e., 2-methyl-2-propanamine) with ethylene oxide, chlorination, cyclization, hydrogenation, debenzylation. The target product was characterized by 1H NMR and MS and its purity was also tested by GC. Exptl. result showed that the reactant in this synthesis route was easily available and it could be applied to industrial production (no data). The experimental process involved the reaction of 2,2′-(tert-Butylazanediyl)diethanol(cas: 2160-93-2).Application of 2160-93-2

The Article related to dimethylethyl piperazine preparation, Heterocyclic Compounds (More Than One Hetero Atom): Pyrazines and Quinoxalines (Including Piperazines) and other aspects.Application of 2160-93-2

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On March 15, 2018, Sato, Takahiro; Nagayama, Yukiho; Yoshino, Yasuhiro; Inoue, Tsutomu; Kato, Hiroshige; Amata, Junichiro; Inaba, Masato; Yamoto, Noriko; Taniguchi, Tetsuya published a patent.HPLC of Formula: 386704-04-7 The title of the patent was Preparation of heterocyclic compounds having erythropoietin-production acceleration activity. And the patent contained the following:

Disclosed are compounds I [X = oxygen atom, nitrogen atom, sulfur atom, etc.; R1-R3 = independently H or alkyl; R4 = H, alkyl or aryl-alkyl; R5 = alkyl, alkenyl, alkynyl, etc. (wherein alkyl, alkenyl and alkynyl are optionally substituted with halo, methoxy, trifluoromethoxy, etc.); or pharmaceutically acceptable salts thereof] and pharmaceutical composition Thus, compound II was prepared via reaction of 2,4-dimethylbenzyl alc. with methanesulfonyl chloride followed by in-situ treatment with [(7-benzyloxy-5-mercapto[1,2,4]triazolo[1,5-a]pyridine-8-carbonyl)amino]acetic acid tert-Bu ester and de-esterification. The invention compounds, e.g., II, promoted erythropoietin (EPO) production in Hep3B cells. Of note, compounds I are useful for the treatment of anemia. The experimental process involved the reaction of (6-(Trifluoromethyl)pyridin-3-yl)methanol(cas: 386704-04-7).HPLC of Formula: 386704-04-7

The Article related to heterocycle preparation erythropoietin production promoter, antianemic agent triazolopyridine erythropoietin production acceleration, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.HPLC of Formula: 386704-04-7

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts

On March 17, 2016, Viet, Andrew Quoc; Wurtz, Nicholas R. published a patent.Recommanded Product: 72364-46-6 The title of the patent was Thioether triazolopyridine and triazolopyrimidine inhibitors of myeloperoxidase. And the patent contained the following:

The invention provides compounds of formula I as myeloperoxidase (MPO) and/or eosinophil peroxidase (EPX) inhibitors, which may be used as medicaments. Compounds of formula I wherein ring A is substituted Ph and (un)substituted 5-to 6-membered heteroaryl; X is CH and N; Y is substituted hydrocarbon linker and substituted hydrocarbon-heteroatom linker; R1 is CN, OH, C1-4 (halo)alkyl, etc. ; and stereoisomers, tautomers, pharmaceutically acceptable salts, polymorphs and solvates thereof, are claimed. Example compound II was prepared by thiolation of 7-chloro-3H-[1,2,3]triazolo[4,5-b]pyridin-5-amine with 1-phenylethylthiol. The invention compounds were evaluated for their myeloperoxidase and/or eosinophil peroxidase inhibitory activity. From the assay, it was determined that compound II exhibited IC50 value ranged from 0.001 μM to 0.01 μM. The experimental process involved the reaction of (2-Fluorophenyl)methanethiol(cas: 72364-46-6).Recommanded Product: 72364-46-6

The Article related to preparation thioether triazolopyridine triazolopyrimidine inhibitor myeloperoxidase eosinophil peroxidase, Heterocyclic Compounds (More Than One Hetero Atom): Other 5-Membered Rings, Two Or More Hetero Atoms and other aspects.Recommanded Product: 72364-46-6

Referemce:
Alcohol – Wikipedia,
Alcohols – Chemistry LibreTexts