Alcohols-buliding-blocks

HPLC of Formula: 2240-88-2On October 14, 2021 ,《Screening Hit to Clinical Candidate: Discovery of BMS-963272, a Potent, Selective MGAT2 Inhibitor for the Treatment of Metabolic Disorders》 was published in Journal of Medicinal Chemistry. The article was written by Turdi, Huji; Chao, Hannguang; Hangeland, Jon J.; Ahmad, Saleem; Meng, Wei; Brigance, Robert; Zhao, Guohua; Wang, Wei; Moore, Fang; Ye, Xiang-Yang; Mathur, Arvind; Hou, Xiaoping; Kempson, James; Wu, Dauh-Rurng; Li, Yi-Xin; Azzara, Anthony V.; Ma, Zhengping; Chu, Ching-Hsuen; Chen, Luping; Cullen, Mary Jane; Rooney, Suzanne; Harvey, Susan; Kopcho, Lisa; Panemangelor, Reshma; Abell, Lynn; O′Malley, Kevin; Keim, William J.; Dierks, Elizabeth; Chang, Shu; Foster, Kimberly; Apedo, Atsu; Harden, David; Dabros, Marta; Gao, Qi; Pelleymounter, Mary Ann; Whaley, Jean M.; Robl, Jeffrey A.; Cheng, Dong; Lawrence, R. Michael; Devasthale, Pratik. The article contains the following contents:

MGAT2 inhibition is a potential therapeutic approach for the treatment of metabolic disorders. High-throughput screening of the BMS internal compound collection identified the aryl dihydropyridinone compound 1 (hMGAT2 IC50 = 175 nM) as a hit. Compound 1 had moderate potency against human MGAT2, was inactive vs mouse MGAT2 and had poor microsomal metabolic stability. A novel chem. route was developed to synthesize aryl dihydropyridinone analogs to explore structure-activity relationship around this hit, leading to the discovery of potent and selective MGAT2 inhibitors 21f, 21s, and 28e that are stable to liver microsomal metabolism After triaging out 21f due to its inferior in vivo potency, pharmacokinetics, and structure-based liabilities and tetrazole 28e due to its inferior channel liability profile, 21s (BMS-963272) was selected as the clin. candidate following demonstration of on-target weight loss efficacy in the diet-induced obese mouse model and an acceptable safety and tolerability profile in multiple preclin. species. After reading the article, we found that the author used 3,3,3-Trifluoropropan-1-ol(cas: 2240-88-2HPLC of Formula: 2240-88-2)

3,3,3-Trifluoropropan-1-ol(cas: 2240-88-2) is a important organic intermediate. It can be used in agrochemical, pharmaceutical and dyestuff field.HPLC of Formula: 2240-88-2

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Application In Synthesis of 4-Butylbenzene-1,2-diolOn November 15, 1990 ,《Stimulatory effect of 4-alkylcatechols and their diacetylated derivatives on the synthesis of nerve growth factor》 appeared in Biochemical Pharmacology. The author of the article were Furukawa, Yoshiko; Fukazawa, Nobuyuki; Miyama, Yukio; Hayashi, Kyozo; Furukawa, Shoei. The article conveys some information:

A series of 4-alkylcatechols and 1,2-diacetoxy-4-alkylbenzenes (Me to Bu) were synthesized for in vitro evaluation as stimulators of nerve growth factor (NGF) synthesis. All compounds were potent in stimulating NGF synthesis in L-M cells (a mouse fibroblast cell line) and mouse astroglial cells. In a series of 4-alkylcatechols, 4-methylcatechol and 4-ethylcatechol severely affected viability and cell adhesive properties. In a series of 1,2-diacetoxy-4-alkylbenzenes, the concentrations required for the maximal effect and the effective ranges of concentrations were higher than those in the 4-alkylcatechol series, and the cell adhesive properties or viabilities were not affected. Evidence is also presented to indicate that the elevation of NGF synthesis by these compounds was not associated with the cell growth. In addition to this study using 4-Butylbenzene-1,2-diol, there are many other studies that have used 4-Butylbenzene-1,2-diol(cas: 2525-05-5Application In Synthesis of 4-Butylbenzene-1,2-diol) was used in this study.

4-Butylbenzene-1,2-diol(cas: 2525-05-5) belongs to organoboron compounds. Organoboron compounds are versatile intermediates and as such are some of the most important classes of reagents in modern organic chemistry. Organoboron compounds are less toxic than organostannane reagents, and unlike alkynylzinc and magnesium, many organoboron compounds possess remarkable oxidative and thermal stabilities. Application In Synthesis of 4-Butylbenzene-1,2-diol

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Recommanded Product: 54-17-1On March 31, 2019, Ye, Luxin; Huang, Binge; Lin, YiJing; Chen, Fan; Li, Jie; Huang, Peng; Sheen, Xiuwei published an article in Latin American Journal of Pharmacy. The article was 《Effect of codeine on urine metabolism in rats》. The article mentions the following:

Codeine, a commonly used cough drug, belongs to opioids, which is used more by drug abusers as an addictive substance. Except tablets, some other preparations of codeine are relatively easy to obtain, and at present in the youth codeine addicts have reached a large number due to cough drug abuse. In order to further comprehend the mechanism of codeine, the effects of codeine on the metabolic pathway of rats were studied by searching the relative relationship between metabolites (urine) and physiol. and pathol. changes. The metabolites were analyzed by gas chromatog.-mass spectrometer, the data were processed by principal component anal. (PCA) and PLS-DA by SIMCA-P 13.0 software, and statistical anal. by SPSS18.0 software. The results indicated that codeine induced metabolic disorder, and Metabolomics could provide a useful tool for the metabolic changes of rats. The results came from multiple reactions, including the reaction of rel-(3R,4S,5S,6R)-6-(Hydroxymethyl)tetrahydro-2H-pyran-2,3,4,5-tetraol(cas: 54-17-1Recommanded Product: 54-17-1)

rel-(3R,4S,5S,6R)-6-(Hydroxymethyl)tetrahydro-2H-pyran-2,3,4,5-tetraol(cas: 54-17-1) is the monohydrate form of the alpha isoform of D-glucopyranose, a synthetic simple monosaccharide that is used as an energy source.Recommanded Product: 54-17-1

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Recommanded Product: (R)-Oxiran-2-ylmethanolOn October 15, 2020 ,《Determining the relative reactivity of sulfate, bisulfate, and organosulfates with epoxides on secondary organic aerosol》 was published in ACS Earth and Space Chemistry. The article was written by Aoki, Erika; Sarrimanolis, Jon N.; Lyon, Sophie A.; Elrod, Matthew J.. The article contains the following contents:

Extensive laboratory and field studies have identified nucleophilic addition reactions of isoprene epoxydiols (IEPOX) as key pathways for the formation of isoprene-derived secondary organic aerosol (SOA). Organosulfates are important reaction products of these processes, but it is unclear whether sulfate and/or bisulfate nucleophiles are responsible for their formation and whether the organosulfates themselves can serve as nucleophiles in oligomer-forming reactions. The relative reactivities (nucleophilic strengths relative to water) of sulfate, bisulfate, and Me sulfate anion were measured through a series of model epoxide-nucleophile experiments using NMR (NMR) spectroscopy. These experiments also helped establish a rigorous understanding of the effects of differing carbon substitution and functional groups of epoxides on the modulation of the effective nucleophilicites of sulfate, bisulfate, and Me sulfate anions. It was determined that the nucleophilicites of bisulfate and Me sulfate anions were about 100 and 50 times, resp., weaker than sulfate toward most of the epoxides studied, which was rationalized by computational estimates of their thermodn. basicities. Therefore, for most SOA acidity situations, sulfate-epoxide reactions are expected to be the main source of organosulfate aerosol constituents. Because sulfate-epoxide reactions stoichiometrically consume acid, these reactions also have the capability of raising the pH of SOA, thus slowing down all acid-catalyzed chem. processes. No evidence for the reaction of the Me sulfate anion was observed with the abundant atmospherically relevant epoxide, trans-β-IEPOX, thus suggesting that oligomerization reactions via epoxide-organosulfate reactions may not be able to compete with stronger (such as sulfate) or more abundant (such as water) nucleophiles on actual SOA.(R)-Oxiran-2-ylmethanol(cas: 57044-25-4Recommanded Product: (R)-Oxiran-2-ylmethanol) was used in this study.

(R)-Oxiran-2-ylmethanol(cas: 57044-25-4) is a chiral building block used to construct an epoxyvinyl iodide intermediate in a synthesis of a furanocembrane, a marine natural product.Recommanded Product: (R)-Oxiran-2-ylmethanol

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Related Products of 6346-09-4On March 20, 2019, Jeppesen, Troels E.; Kristensen, Lotte K.; Nielsen, Carsten H.; Petersen, Lars C.; Kristensen, Jesper B.; Behrens, Carsten; Madsen, Jacob; Kjaer, Andreas published an article in Bioconjugate Chemistry. The article was 《Oxime Coupling of Active Site Inhibited Factor Seven with a Nonvolatile, Water-Soluble Fluorine-18 Labeled Aldehyde》. The article mentions the following:

A nonvolatile fluorine-18 aldehyde prosthetic group was developed from [18F]SFB, and used for site-specific labeling of active site inhibited factor VII (FVIIai). FVIIai has a high affinity for tissue factor (TF), a transmembrane protein involved in angiogenesis, proliferation, cell migration, and survival of cancer cells. A hydroxylamine N-glycan modified FVIIai (FVIIai-ONH2) was used for oxime coupling with the aldehyde [18F]2 under mild and optimized conditions in an isolated RCY of 4.7 ± 0.9%, and a synthesis time of 267 ± 5 min (from EOB). Retained binding and specificity of the resulting [18F]FVIIai to TF was shown in vitro. TF-expression imaging capability was evaluated by in vivo PET/CT imaging in a pancreatic human xenograft cancer mouse model. The conjugate showed exceptional stability in plasma (>95% at 4 h) and a binding fraction of 90%. In vivo PET/CT imaging showed a mean tumor uptake of 3.8 ± 0.2% ID/g at 4 h post-injection, a comparable uptake in liver and kidneys, and low uptake in normal tissues. In conclusion, FVIIai was labeled with fluorine-18 at the N-glycan chain without affecting TF binding. In vitro specificity and a good in vivo imaging contrast at 4 h postinjection was demonstrated. In the part of experimental materials, we found many familiar compounds, such as 4,4-Diethoxybutan-1-amine(cas: 6346-09-4Related Products of 6346-09-4)

4,4-Diethoxybutan-1-amine(cas: 6346-09-4) belongs to anime. Amine, any member of a family of nitrogen-containing organic compounds that is derived, either in principle or in practice, from ammonia (NH3). Naturally occurring amines include the alkaloids, which are present in certain plants; the catecholamine neurotransmitters (i.e., dopamine, epinephrine, and norepinephrine); and a local chemical mediator, histamine, that occurs in most animal tissues.Related Products of 6346-09-4

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Formula: C8H9NO5SOn September 3, 2019 ,《Conjugation of Antibodies to Horseradish Peroxidase.》 was published in Cold Spring Harbor protocols. The article was written by Berg, Eric A; Fishman, Jordan B. The article contains the following contents:

Antibodies conjugated with horseradish peroxidase (HRP) are one of the most widely used bioreagents in the biological sciences. This protocol is a basic method for adding HRP to a thiolated antibody and can be adapted for use with different cross-linkers. Conjugation methods usually focus on linking through the lysines on HRP because there are only six of them and their modification does not adversely affect enzyme activity. The experimental process involved the reaction of 2,5-Dioxopyrrolidin-1-yl 2-(acetylthio)acetate(cas: 76931-93-6Formula: C8H9NO5S)

2,5-Dioxopyrrolidin-1-yl 2-(acetylthio)acetate(cas: 76931-93-6) belongs to pyrrolidine. Pyrrolidine being a good nucleophile easily undergoes electrophilic substitution reactions with different electrophiles such alkyl halides and acyl halides, and forms N-substituted pyrrolidines. N-Alkylpyrrolidine on further reaction with alkyl halide provided quaternary salts.Formula: C8H9NO5S

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In 1954,Nippon Nogei Kagaku Kaishi included an article by Okuma, Kazuhiko; Tamura, Saburo. COA of Formula: C10H14O2. The article was titled 《Inhibition of the autoxidation of fats and oils. XI. Syntheses of some ω-(2,5-dihydroxyphenyl)alkanoic esters and ω,ω’-bis(2,5-dihydroxyphenyl)alkanes》. The information in the text is summarized as follows:

Since hydroquinone derivatives seemed to have generally higher antioxidant activity than catechol derivatives, the 2,5-dihydroxyphenyl derivatives rather than 3,4-dihydroxyphenyl derivatives were synthesized as possible antioxidants. Me-γ-(2,5-dihydroxyphenyl)butyrate (X) was obtained by esterifying the corresponding free acid (XI). Fieser, et al. (C.A. 35, 889), could not prepare XI by demethylation of γ-(2,5-dimethoxyphenyl)butyric acid. This was presumed to be due to cyclization. β-(2,5-Dimethoxybenzoyl)propionic acid (XII), m. 101-2°, prepared according to F., et al. (loc. cit.), was demethylated with HI to β-(2,5-dihydroxybenzoyl)propionic acid (XIII), m. 180-2°, yellow columns in 81% yield. XIII was hydrogenated with Zn-Hg to XI, m. 131-2°, in low yield (1 g. from 20 g. XIII). XI (0.3 g.) refluxed with MeOH and H2SO4 gave 71.8% X, m. 66-7°, tabular crystals. XII (10 g.) demethylated with 13 g. AlCl3 and 100 cc. PhCl did not give XIII, but β-(2-hydroxy-5-methoxybenzoyl)propionic acid, m. 140° [the positions of OH and OMe in the benzene nucleus were not determined, but were assumed by analogy to the formation of 2-hydroxy-5-methoxy-β-chlorochalcone (Simonis and Danishevski, C.A. 21, 1255]). Hydroquinone di-Me ether (69 g.) with polymeric adipic anhydride, m. 75° (prepared from 73 g. adipic acid and 300 cc. Ac2O), in the presence of 140 g. AlCl3 gave 55 g. δ-(2,5-dimethoxybenzoyl)valeric acid, m. 78-80°, needles, 30 g. of which hydrogenated with 72 g. Zn amalgam gave 14.7 g. ε-(2,5-dimethoxyphenyl)hexanoic acid, b5 200-2°, m. 64-7°. This was demethylated with HI to give ε-(2,5-dihydroxyphenyl)hexanoic acid, m. 112-13° [m. 96.8-97.6°, by Fieser, et al. (loc. cit.), but the analysis conformed with the theoretical]. This was methylated to give Me ester, which could not be crystallized (analysis differed somewhat from the theoretical). Hydroquinone di-Me ether (30 g.) with 14.6 g. adipic acid and 25 cc. SOCl2 gave 12 g. 1,4-bis(2,5-dimethoxybenzoyl)butane, m. 105-6°, needles, 5 g. of which with 2.5 cc. 80% hydrazine hydrate gave 3.7 g. yellow 1,6-bis(2,5-dimethoxyphenyl)hexane. This was not purified, but was demethylated with HI to give 1,6-bis(2,5-dihydroxyphenyl)hexane, m. 159-60°, scales. Similarly, 1,10-bis(2,5-dihydroxyphenyl)decane, m. 148-50°, scales, was obtained in 46.3% yield by demethylation with HI of 1,10-bis(2,5-dimethoxyphenyl)decane, m. 76-8°, needles, in 56.2% yield from 1,8-bis(2,5-dimethoxybenzoyl)octane, m. 99-100°, needles, prepared from hydroquinone di-Me ether and sebacoyl chloride. The experimental process involved the reaction of 4-Butylbenzene-1,2-diol(cas: 2525-05-5COA of Formula: C10H14O2)

4-Butylbenzene-1,2-diol(cas: 2525-05-5) belongs to organoboron compounds. Organoboron compounds are versatile intermediates and as such are some of the most important classes of reagents in modern organic chemistry.COA of Formula: C10H14O2 Organoboron compounds are less toxic than organostannane reagents, and unlike alkynylzinc and magnesium, many organoboron compounds possess remarkable oxidative and thermal stabilities.

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Le, Thuy G.; Kundu, Abhijit; Ghoshal, Atanu; Nguyen, Nghi H.; Preston, Sarah; Jiao, Yaqing; Ruan, Banfeng; Xue, Lian; Huang, Fei; Keiser, Jennifer; Hofmann, Andreas; Chang, Bill C. H.; Garcia-Bustos, Jose; Wells, Timothy N. C.; Palmer, Michael J.; Jabbar, Abdul; Gasser, Robin B.; Baell, Jonathan B. published an article on January 24 ,2019. The article was titled 《Structure-activity relationship studies of tolfenpyrad reveal subnanomolar inhibitors of Haemonchus contortus development》, and you may find the article in Journal of Medicinal Chemistry.SDS of cas: 2240-88-2 The information in the text is summarized as follows:

Recently, we have discovered that the registered pesticide, tolfenpyrad, unexpectedly and potently inhibits the development of the L4 larval stage of the parasitic nematode Haemonchus contortus with an IC50 value of 0.03 μM while displaying good selectivity, with an IC50 of 37.9 μM for cytotoxicity. As a promising mol. template for medicinal chem. optimization, we undertook anthelmintic structure-activity relationships for this chem. Modifications of the left-hand side (LHS), right-hand side (RHS), and middle section of the scaffold were explored to produce a set of 57 analogs. Analogs I, II, and III were shown to be the most potent compounds of the series, with IC50 values at a subnanomolar level of potency against the chemotherapeutically relevant fourth larval (L4) stage of H. contortus. Selected compounds from the series also showed promising activity against a panel of other different parasitic nematodes, such as hookworms and whipworms. In the part of experimental materials, we found many familiar compounds, such as 3,3,3-Trifluoropropan-1-ol(cas: 2240-88-2SDS of cas: 2240-88-2)

3,3,3-Trifluoropropan-1-ol(cas: 2240-88-2) is a important organic intermediate. It can be used in agrochemical, pharmaceutical and dyestuff field.SDS of cas: 2240-88-2

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Lewin, Anita H.; Brieaddy, Larry; Deschamps, Jeffrey R.; Imler, Gregory H.; Mascarella, S. Wayne; Reddy, P. Anantha; Carroll, F. Ivy published an article on January 16 ,2019. The article was titled 《Synthesis and Characterization of the Selective, Reversible PKCβ Inhibitor (9S)-9-[(Dimethylamino)methyl]-6,7,10,11-tetrahydro-9H,18H-5,21:12,17-dimethenodibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecine-18,20(19H)-dione, Ruboxistaurin (LY333531)》, and you may find the article in ACS Chemical Neuroscience.Reference of (R)-Oxiran-2-ylmethanol The information in the text is summarized as follows:

The demonstrated role of PKCβ in mediating amphetamine-stimulated dopamine efflux, which regulates amphetamine-induced dopamine transporter trafficking and activity, has promoted the research use of the selective, reversible PKCβ inhibitor (9S)-9-[(dimethylamino)methyl]-6,7,10,11-tetrahydro-9H,18H-5,21:12,17-dimethenodibenzo[e,k]pyrrolo[3,4-h][1,4,13]oxadiazacyclohexadecine-18,20(19H)-dione, ruboxistaurin. Despite the interest in development of ruboxistaurin as the mesylate monohydrate (Arxxant) for the treatment of diabetic retinopathy, macular edema, and nephropathy, several crucial details in physicochem. characterization were erroneous or missing. This report describes the synthesis and full characterization of ruboxistaurin free base (as a monohydrate), including X-ray crystallog. to confirm the absolute configuration, and of the mesylate salt, isolated as a hydrate containing 1.5 mol of water per mol.(R)-Oxiran-2-ylmethanol(cas: 57044-25-4Reference of (R)-Oxiran-2-ylmethanol) was used in this study.

(R)-Oxiran-2-ylmethanol(cas: 57044-25-4) is a chiral building block used to construct an epoxyvinyl iodide intermediate in a synthesis of a furanocembrane, a marine natural product.Reference of (R)-Oxiran-2-ylmethanol

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The author of 《Concise and efficient syntheses of methyl 4-(1-methylpyrrolidin-2-yl)-3-oxobutanoate and hygrine》 were Ma, Xiao-Yan; Huang, Jian-Ping; Yang, Jing; Liu, Xingyong; Hu, Xinjun; Huang, Sheng-Xiong. And the article was published in Canadian Journal of Chemistry in 2020. Safety of 4,4-Diethoxybutan-1-amine The author mentioned the following in the article:

Me 4-(1-methylpyrrolidin-2-yl)-3-oxobutanoate and hygrine are important biosynthetic intermediates for tropane alkaloids. A concise method to synthesize these two compounds from the key intermediate N-methylpyrrolinium cation has been developed. Me 4-(1-methylpyrrolidin-2-yl)-3-oxobutanoate and hygrine were obtained in four and six steps from com. available 4,4-diethoxybutylamine with overall yields of 42% and 25%, resp. In the experiment, the researchers used 4,4-Diethoxybutan-1-amine(cas: 6346-09-4Safety of 4,4-Diethoxybutan-1-amine)

4,4-Diethoxybutan-1-amine(cas: 6346-09-4) belongs to anime. Left-handed and right-handed forms (mirror-image configurations, known as optical isomers or enantiomers) are possible when all the substituents on the central nitrogen atom are different (i.e., the nitrogen is chiral). With amines, there is extremely rapid inversion in which the two configurations are interconverted.Safety of 4,4-Diethoxybutan-1-amine

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