CAS: 5834-16-2; 3-Methyl-2-Thiophenecarboxaldehyde ,Tech

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CAS号68-12-2 N,N-二甲基甲酰胺 | CAS号616-44-4 3-甲基噻吩 | CAS号13207-03-9 methyl α-acetox... | CAS号89055-55-0 [1-(1,3-dioxola... | CAS号4885-02-3 1,1-二氯甲醚 | CAS号93-61-8 N-甲基甲酰苯胺 | CAS号3760-54-1 1-甲酰吡咯烷 | CAS号2591-86-8 1-甲酰哌啶 | CAS号2861-59-8 1-甲酸基吲哚啉 | CAS号2700-30-3 二异丙基甲酰胺 | CAS号41056-90-0 3-甲硫基苯e-2-甲醛肟 | CAS号145821-58-5 噻加宾乙酯 | CAS号30717-55-6 双(3-甲基噻吩-2-基)甲酮 | CAS号55406-13-8 3-甲基噻吩-2-腈 | CAS号632-16-6 2,3-二甲基噻吩 | CAS号63826-56-2 (3-甲基噻吩-2-基)甲醇 | CAS号5928-48-3 4,5-二甲基噻吩-2-羧醛 | CAS号76655-99-7 3-甲基噻吩-2-羧酰胺 | CAS号102696-70-8 (E)-3-(3-甲基噻吩-2... | CAS号104085-30-5 2-{[3-(溴甲基)-2-噻...

2,3-二甲基噻吩置于三氯氧磷体系中,用 N,N-二甲基甲酰胺 作为反应溶剂,化学反应 8.0H,以89%的收率获得产物3-甲基噻吩醛
参考文献:二芳基甲烷骨架的系统构效关系 (Sar) 探索和高效新型尿酸转运蛋白 1 (Urat1) 抑制剂的发现
标题:二芳基甲烷骨架的系统构效关系 (Sar) 探索和高效新型尿酸转运蛋白 1 (Urat1) 抑制剂的发现
摘要:为了系统地探索和更好地理解二芳基甲烷骨架在设计强效尿酸转运蛋白 1 (Urat1) 抑制剂时的构效关系 (Sar),设计并合成了 33 种化合物(1A-1X 和 1Ha-1Hi),并测定了它们的体外 Urat1 抑制活性 (Ic50).三轮系统的 Sar 探索导致发现了一种高效的新型 Urat1 抑制剂,1H,其效力分别比母体 Lesinurad 和苯溴马隆强 200 倍和 8 倍(ic50 = 0.035 μm 对人 Urat1 1 小时 Vs Lesinurad 和苯溴马隆分别为 7.18 μm 和 0.28 μm).化合物 1H 是迄今为止我们实验室发现的最有效的 Urat1 抑制剂,也可与目前正在临床试验中开发的最有效的抑制剂相媲美.
DOI:10.3390/molecules23020252

专利信息

专利号:WO-2008115912-A1
优先权日:2007-03-21
标题:Regio-specific synthesis of 4-bromo-3-methyl-5-propoxy-thiophene-2-carboxylic acid
发明人：KUBIAK GREGORY G; LYTHGOE DAVID J; YU YONG
权利人:SANOFI AVENTIS; KUBIAK GREGORY G; LYTHGOE DAVID J; YU YONG
摘要:This invention is directed to a five step regio-specific synthesis of 4-bromo-3-methyl-5-propoxy-thiophene-2-carboxylic acid compound of formula 16 comprising the steps of acetalating 3-methyl-thiophene-2-carbaldehyde in an alcohol solvent; iodinating the acetalated 3-methyl-thiophene-2-carbaldehyde in an non-protic polar or hydrocarbon solvent to yield the corresponding iodinated and acetalated 3-methyl-thiophene-2-carbaldehyde product; treating the iodinated and acetalated product with water to yield the corresponding 5-iodo-3-methyl-thiophene-2-carbaldehyde; oxidizing the 5-iodo-3-methyl-thiophene-2-carbaldehyde to the corresponding 5-iodo-3-methyl-thiophene-2-carboxylic acid in ketone solvent; Ullmann coupling of the 5-iodo-3-methyl-thiophene-2-carboxylic acid with alkali metal propoxide salt using a copper catalyst in propanol to yield 3-methyl-5-propoxy-thiophene-2-carboxylic acid; esterifying 3-methyl-5-propoxy-thiophene-2-carboxylic acid to yield the corresponding alkyl 3-methyl-5-propoxy-thiophene-2-carboxylate; brominating the 3-methyl-5-propoxy-thiophene-2-carboxylic acid to yield the corresponding alkyl 4-bromo-3-methyl-5-propoxy-thiophene-2-carboxylate; and basic hydrolyzing the alkyl 4-bromo-3-methyl-5-propoxy-thiophene-2-carboxylate with base to yield 4-bromo-3-methyl-5-propoxy-thiophene-2-carboxylic acid.

专利号:WO-2008121666-A1
优先权日:2007-03-29
标 题 :Use of 4-bromo-3-methyl-5-propoxythiophene-2-carboxylic acid 2,5-dioxo-pyrrolidin-1-yl ester for preparing the tryptase inhibitor [4-(5-aminomethyl-2-fluoro-phenyl)-piperidin-1-yl]-(4-bromo-3-methyl-5-propoxy-thiophen-2-yl)-methanone
发明人：GELORMINI ANN MARIE; SLEDESKI ADAM W; SHAY JOHN JOSEPH JR
权利人:SANOFI AVENTIS; GELORMINI ANN MARIE; SLEDESKI ADAM W; SHAY JOHN JOSEPH JR
摘要:This invention is directed to a five step regio-specific synthesis of 4-bromo-3-methyl-5-propoxy-thiophene-2-carboxylic acid compound of formula 16 comprising the steps of acetalating 3-methyl-thiophene-2-carbaldehyde in an alcohol solvent; iodinating the acetalated 3-methyl-thiophene-2-carbaldehyde in an non-protic polar or hydrocarbon solvent to yield the corresponding iodinated and acetalated 3-methyl-thiophene-2-carbaldehyde product; treating the iodinated and acetalated product with water to yield the corresponding 5-iodo-3-methyl-thiophene-2-carbaldehyde; oxidizing the 5-iodo-3-methyl-thiophene-2-carbaldehyde to the corresponding 5-iodo-3-methyl-thiophene-2-carboxylic acid in ketone solvent; Ullmann coupling of the 5-iodo-3-methyl-thiophene-2-carboxylic acid with alkali metal propoxide salt using a copper catalyst in propanol to yield 3-methyl-5-propoxy-thiophene-2-carboxylic acid; esterifying 3-methyl-5-propoxy-thiophene-2-carboxylic acid to yield the corresponding alkyl 3-methyl-5-propoxy-thiophene-2-carboxylate; brominating the 3-methyl-5-propoxy-thiophene-2-carboxylic acid to yield the corresponding alkyl 4-bromo-3-methyl-5-propoxy-thiophene-2-carboxylate; and basic hydrolyzing the alkyl 4-bromo-3-methyl-5-propoxy-thiophene-2-carboxylate with base to yield 4-bromo-3-methyl-5-propoxy-thiophene-2-carboxylic acid.

专利号:US-5175302-A
优先权日:1987-07-13
标 题 :Nucleophilic fluoroalkylation of aldehydes
发明人：STAHLY G PATRICK
权利人:ETHYL CORP
摘要:Aryl difluoromethyl sulfone adds to aldehydes under phase transfer conditions to give novel substituted alcohols of the general formula n n RCH(OH)CF.sub.2 SO.sub.2 Ar (I) n n wherein R is an aryl, cycloaliphatic, sec- or tert-aliphatic, or heterocyclic group and Ar is an aryl group. The substituted alcohols of formula I are of particular utility as intermediates in the synthesis of a variety of useful end products. For example, the products of formula I may be utilized in desulfonylation reactions, oxidation reactions and fluorination reactions.

专利号:US-4837327-A
优先权日:1987-07-13
标 题 :Process for nucleophilic fluoroalkylation of aldehydes
发明人：STAHLY G PATRICK
权利人:ETHYL CORP
摘要:Aryl difluoromethyl sulfone adds to alkehydes under phase transfer conditions to give novel substituted alcohols of the general formula n n RCH(OH)CF.sub.2 SO.sub.2 Ar (I) n n wherein R is an aryl, cycloaliphatic, sec- or tert-aliphatic, or heterocyclic group and Ar is an aryl group. The substituted alcohols of formula I are of particular utility as intermediates in the synthesis of a variety of useful end products. For example, the products of formula I may be utilized in desulfonylation reactions, oxidation reactions and fluorination reactions.

专利号:US-4999429-A
优先权日:1989-01-09
标 题 :Process for the preparation of α,α,β-1-trifluoro-1-olefinic derivatives
发明人：STAHLY G PATRICK
权利人:ETHYL CORP
摘要:Aryl difluoromethyl sulfone adds to aldehydes under phase transfer conditions to give novel substituted alcohols of the general formula n n RCH(OH)CF.sub.2 SO.sub.2 Ar (I) n n wherein R is an aryl, cycloaliphatic, sec- or tert-aliphatic, or heterocyclic group and Ar is an aryl group. The substituted alcohols of formula I are of particular utility as intermediates in the synthesis of a variety of useful end products. For example, the products of formula I may be utilized in desulfonylation reactions, oxidation reactions and fluorination reactions.

专利号:US-2023192718-A1
优先权日:2018-03-30
标 题 :Bicyclic enone carboxylates as modulators of transporters and uses thereof
发明人：SANDANAYAKA VINCENT
权利人:NIROGY THERAPEUTICS INC
摘要:The invention generally relates to the field of monocarboxylate transporter inhibitors, and more particularly to new bicyclic enone carboxylate enone compounds, the synthesis and use of these compounds and their pharmaceutical compositions, e.g., in the treatment, modulation and/or prevention of physiological conditions associated with monocarboxylate transporter activity such as in treating cancer and other neoplastic disorders, tissue and organ transplant rejection.