3-甲基噻吩置于alkaline Aqueous Alkali Hypoiodite Solution,Boron Fluoride Ether体系中,化学反应生成3-甲基噻吩-2-羧酸 参考文献:Condensations Effected By Boron Fluoride Complexes. Iii. The Acylation Of Certain Substituted Thiophenes And Furans1 标题:Condensations Effected By Boron Fluoride Complexes. Iii. The Acylation Of Certain Substituted Thiophenes And Furans1 摘要: Doi:10.1021/ja01164A103
专利号:US-2021107859-A1 优先权日:2018-04-06 标题 :A process for the synthesis of carbon labeled organic compounds 发明人:AUDISIO DAVIDE; CANTAT THIBAULT; DESTRO GIANLUCA 权利人:COMMISSARIAT ENERGIE ATOMIQUE 摘要:A process for the synthesis of a carbon labeled organic compound containing a carbon labeled carboxyl group is described. A method of using carbon labeled organic compounds containing a carbon labeled carboxyl group according to the present disclosure; a process for manufacturing labeled pharmaceuticals and agrochemicals comprising synthesis of carbon labeled organic compounds containing a carbon labeled carboxyl group according to the present disclosure; and a process for producing tracers comprising synthesis of carbon labeled organic compounds containing a carbon labeled carboxyl group according to the present disclosure are also described.
专利号:WO-2008109786-A3 优先权日:2007-03-07 标题:Regio-selective ullmann synthesis of 4-bromo-3-methyl-5-propoxy-thiophene-2-carboxylic acid 发明人:AYERS TIMOTHY A; GELORMINI ANN MARIE; SHAY JOHN J JR; SLEDESKI ADAM W; YU YONG 权利人:SANOFI AVENTIS; AYERS TIMOTHY A; GELORMINI ANN MARIE; SHAY JOHN J JR; SLEDESKI ADAM W; YU YONG 摘要:This invention is directed to a two step regio-selective Ullmann synthesis of 4-bromo-3- methyl-5-propoxy-thiophene-2-carboxylic acid compound of formula 16 comprising the steps of brominating 3-methyl-thiophene-2-carboxylic acid to yield 4,5-dibromo-3-methyl- thiophene-2-carboxylic acid in appropriate bromination organic solvent, and then effecting the selective Ullmann coupling of the 4,5-dibromo-3-methyl-thiophene-2-carboxylic cid with alkali metal propoxide salt using copper catalyst in propanol to yield the compound of formula 16.
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:US-2024199637-A1 优先权日:2021-04-21 标题 :Improved process for the preparation of 7-(morpholinyl)-2-(n-piperazinyl)methylthieno[2, 3-c]pyridine derivatives 发明人:KOMPELLA AMALA; VAGICHERLA KAMESWARA RAO; LANKI REDDY TIRUMALA REDDY; PESARU NARMADA; MUDDASANI PULLA REDDY; NANNAPANENI VENKAIAH CHOWDARY 权利人:NATCO PHARMA LTD 摘要:The present invention describes an improved second generation process for the synthesis of NRC-1111 (1,5-[2-[[4-(methylsulfonyl)-1-piperazinyl]methyl]-7-(4-morpholinyl)thieno[2,3-c] pyridine-5-yl]-2-pyrimidinamine) dimethane sulfonate and NRC-1109 (II, 5-[3-methyl-2-[(4-methylsulfonylpiperazin-1-yl)methyl]-7-morpholino-thieno[2,3-c]pyridin-5-yl]pyrimidin-2-amine) dimethane sulfonate. This process is cost effective, high yielding and industrially feasible process for the synthesis of compounds of formulae I and II with high purity. Formula (I) Formula (I): Râ•?H for NRC-1111 and Formula (II): Râ•?CH3 for NRC-1109 NRC-1111 and NRC-1109 are potential anti-cancer agents.
专利号:US-6281391-B1 优先权日:1998-10-27 标 题 :Synthesis of methylthiophenyl hydroxyketones 发明人:TILLYER RICHARD D; DAVIES IAN W; LARSEN ROBERT D; WANG XIN; O'SHEA PAUL; KING ANTHONY ON-PING; ZHAO DALIAN; CHEN CHENG Y; GRABOWSKI EDWARD J J 权利人:MERCK & CO INC; MERCK FROSST CANADA INC 摘要:This invention encompasses a novel process for synthesizing compounds represented by formula A: n These compounds are intermediates useful in the preparation of certain agents that are selective COX-2 inhibitors.
专利号:EP-3515880-B1 优先权日:2017-03-17 标题:Methods and compositions for synthesis of encoded libraries 发明人:LI JIN; MORGAN BARRY A; Wan jinqiao; DOU DENGFENG; LIU GUANSAI; CHANG YONG; CHEN QIUXIA; WANG XING; XU YANSHAN; HU DONGYAN; LIU JIAN; CHENG XUEMIN 权利人:HITGEN INC
摘要:Zhang, M.; Su, W., Science of Synthesis: Cross Coupling and Heck-Type Reactions, (2012) 3, 113. 摘要:Lai, J.; Thomson, B. J.; Sammis, G. M., Science of Synthesis: Modern Strategies in Organofluorine Chemistry , (2024) 1, 28.