发明名称 Process for the manufacture of 4-fluoro-2-methyl-1H-indol-5-ol
摘要 The present invention relates to a chemical process for the manufacture of a compound of Formula II;
申请公布号 US8754240(B2) 申请公布日期 2014.06.17
申请号 US201012948310 申请日期 2010.11.17
申请人 AstraZeneca AB 发明人 Arnott Euan Alexander;Crosby John;Evans Mathew Charles;Ford James Gair;Jones Martin Francis;Leslie Kevin William;McFarlane Ian Michael;Sependa George Joseph
分类号 C07D209/04 主分类号 C07D209/04
代理机构 Morgan, Lewis & Bockius LLP 代理人 Morgan, Lewis & Bockius LLP
主权项 1. A process for the manufacture of a compound of Formula IIthe process comprising the steps of: (a) in the presence of a solvent, reacting a compound of Formula III: wherein R1 and R2 are independently selected from the group consisting of chlorine, bromine, fluorine, iodine, triflyl and tosyl; with an ester of Formula IV wherein R3 isC1-6alkyl or benzyl;to form a compound of Formula V: (b) in the presence of an arylalkyl ammonium salt or a tetraalkyl ammonium salt, reacting a compound of Formula V with hydroxide ion to form a compound of Formula VI (c) in the presence of an acid, decarboxylating a compound of Formula VI to form a compound of Formula VII; and (d) reducing the compound of Formula VII to form the compound of Formula II.
地址 Sodertalje SE