CAS: 22288-78-4; Methyl 3-Amino-2-Thiophenecarboxylate

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3-氧基四氢噻吩-2-羧酸甲酯置于盐酸羟胺体系中,用 水,乙腈 用作溶剂,化学反应生成3-氨基-2-噻吩甲酸甲酯
参考文献:Process For Preparing Thiophene Derivatives
标题:Process For Preparing Thiophene Derivatives
摘要:一种制备3-氨基噻吩或其酸加成盐的方法,包括在极性惰性溶剂存在且无碱存在的情况下,将相应的3-氧代四氢噻吩与羟胺酸加成盐反应,在0oc至200oc的温度范围内进行.

专利信息

专利号:US-11999749-B2
优先权日:2021-06-30
标题 :Synthesis of a bis-mesylate salt of 4-amino-N-(1-((3-chloro-2-fluorophenyl)amino)-6-methylisoquinolin-5-yl)thieno[3,2-d]pyrimidine-7-carboxamide and intermediates thereto
发明人：GOSSELIN FRANCIS; KOENIG STEFAN G; MERCADO-MARIN EDUARDO V; STUMPF ANDREAS; ZELL DANIEL; ZHANG HAIMING; BACHMANN STEPHAN; CARRERA DIANE E; DALZIEL MICHAEL E; GE YONGHUI; ZHANG JIE; BIGLER RAPHAEL; FINET LAURE ELIZABETH SIMONE; MONDIERE REGIS JEAN GEORGES; NAKAGAWA YUKI
权利人:GENENTECH INC; HOFFMANN LA ROCHE
摘要:A manufacturing process to a bis-mesylate salt 1b of the pan-RAF inhibitor 4-amino-n-(1-((3-chloro-2-fluorophenyl)amino)-6-methylisoquinolin-5-yl)thieno[3,2-d]pyrimidine-7-carboxamide. The process features a number of efficient key reactions, including a robust and scalable Pd-catalyzed carbonylation reaction to generate thienopyrimidine 2 and a highly chemoselective Pt/V/C-catalyzed nitro group reduction to access penultimate intermediate 7. The final amide coupling of 7 and 2 was accomplished by a mild and safe protocol employing N,N,N′,N′-tetramethylchloroformamidinium hexafluorophosphate (TCFH) as the coupling reagent, to produce a 1:1 adduct of the freebase and THF. The adduct afforded compound 1b with excellent yield, purity, and form stability on a multikilogram production scale after reaction with MsOH and recrystallization. The methods are able to produce a compound having upwards of 95% purity.

专利号:US-9895374-B2
优先权日:2015-03-02
标 题:Thieno- and pyrrolopyrimidine analogues as anticancer agents and methods of use thereof
发明人：RADTKE KATHERINE L; TEMBURNIKAR KARTIK
权利人:UNIV MARYLAND
摘要:The present invention provides for the design and synthesis of halogenated thieno- and pyrrolopyrimidine compounds that exhibit cancer proliferation inhibitory activity and the use thereof for cancer treatment.

专利号:US-4897484-A
优先权日:1986-12-19
标题 :Process for the preparation of substituted pyridines
发明人：WEIS CLAUS D; SUTTER PETER
权利人:CIBA GEIGY CORP
摘要:A process is described for the preparation of compounds of the formula (1) in which R and X are as defined in claim 1. The compounds of the formula (1) are valuable intermediates in the synthesis of triarylmethane dyes and triarylmethanelactones.

专利号:US-10646490-B2
优先权日:2015-03-02
标 题 :Thieno- and pyrrolopyrimidine analogues and prodrugs thereof as anticancer agents and methods of use thereof
发明人：RADTKE KATHERINE L
权利人:UNIV MARYLAND
摘要:The present invention provides for the design and synthesis of halogenated thieno- and pyrrolopyrimidine compounds and prodrugs thereof that exhibit cancer proliferation inhibitory activity and the use thereof for cancer treatment.

专利号:US-6531470-B1
优先权日:1998-01-23
标题:Oxazolidinone combinatorial libraries, compositions and methods of preparation
发明人：GORDEEV MIKHAIL F; LUEHR GARY W; PATEL DINESH V; NI ZHI-JIE; GORDON ERIC
权利人:UPJOHN CO
摘要:Oxazolidinones and methods for their synthesis are provided. Also provided are combinatorial libraries comprising oxazolidinones, and methods to prepare the libraries. Further provided are methods of making biologically active oxazolidinones as well as pharmaceutically acceptable compositions comprising the oxazolidinones. The methods of library preparation include the attachment of oxazolidinones to a solid support. The methods of compound preparation in one embodiment involve the reaction of an iminophosphorane with a carbonyl containing polymeric support.

专利号:US-2025051351-A1
优先权日:2021-06-30
标题 :Synthesis of a bis-mesylate salt of 4-amino-n-(1-((3-chloro-2-fluorophenyl)amino)-6-methylisoquinolin-5-yl)thieno[3,2-d]pyrimidine-7-carboxamide and intermediates thereto