CAS: 2106-04-9; 3-Chloro-2-Fluoroaniline

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2,3-二氯硝基苯置于potassium Fluoride,铁粉,N,N-二甲基甲酰胺体系中,化学反应生成3-氯-2-氟苯胺
参考文献:Aromatic Fluorine Compounds. Viii. Plant Growth Regulators And Intermediates1,2
标题:Aromatic Fluorine Compounds. Viii. Plant Growth Regulators And Intermediates1,2
摘要:
Doi:10.1021/ja01510A021

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-8993753-B2
优先权日:2009-08-06
标题:Stereoselective synthesis of bicyclic heterocycles
发明人：OSTERMEIER MARKUS; DAEUBLER JUERGEN; HUCHLER GUENTHER; KLING STEPHAN; SANTAGOSTINO MARCO
权利人:OSTERMEIER MARKUS; DAEUBLER JUERGEN; HUCHLER GUENTHER; KLING STEPHAN; SANTAGOSTINO MARCO; BOEHRINGER INGELHEIM INT
摘要:The present invention relates to a process for the stereoselective preparation of compounds of formulae (1A) and (1B) n nand the salts thereof, particularly the physiologically acceptable salts thereof with inorganic or organic acids and bases, which have valuable pharmacological properties, particularly an inhibitory effect on signal transduction mediated by tyrosine kinases, the use thereof for the treatment of diseases, particularly tumoral diseases as well as benign prostatic hyperplasia (BPH), diseases of the lungs and airways.

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

专利号:US-2023028651-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

专利号:TW-202311265-A
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

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