发明名称 Methods for preparing intermediates of perampanel
摘要 Methods for the synthesis of 2-alkoxy-5-(pyridin-2-yl)pyridine of formula I; or salts thereof are provided.
申请公布号 US8742118(B2) 申请公布日期 2014.06.03
申请号 US201213654437 申请日期 2012.10.18
申请人 F.I.S.—Fabbrica Italiana Sintetici S.p.A. 发明人 Fontana Francesco;Stabile Paolo
分类号 C07D213/22;A61K31/44 主分类号 C07D213/22
代理机构 代理人
主权项 1. A method for the preparation of 2-alkoxy-5-(pyridin-2-yl)pyridine of formula (I) or of a salt thereof: wherein R is a linear or branched C1-C6 alkyl group, comprising the following steps: (a) converting of a 5-halogen-2-alkoxypyridine of formula (IV) wherein X is selected from the group consisting of: chlorine, bromine and iodine and R is a linear or branched C1-C6 alkyl group, into a halide of (6-alkoxypyridin-3-yl)magnesium of formula (III) or in a lithium chloride complex thereof of formula all-bis): wherein X′ is selected from the group consisting of: chlorine, bromine and iodine, (b) reacting of the compound obtained in the step (a) with a 2-halogenpyridine or 2-pseudohalogenpyridine of formula (II) wherein X′ is selected from the group consisting of: chlorine, bromine, iodine, triflate, nonaflate, mesylate, tosylate and besylate or —O(C═O)NR′2 and wherein R′ is a linear or branched C1-C4 alkyl group or is phenyl or benzyl, to provide the compound of formula (I) or a salt thereof.
地址 Alte di Montecchio Maggiore (VI) IT