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邻氟溴苄(14)与水合肼缩合,再与氰基丙酮酸钠盐(3)反应环合得到5-氨基-1-(2-氟苄基)吡唑-3-甲酸乙酯(4),4与1,1,3,3-四甲氧基丙烷反应,再经一系列的官能团转化反应得到1-(2-氟苄基)-1H-吡唑并[3,4-b]吡啶-3-甲脒盐酸盐(9′),9′与苯偶氮丙二腈(10)经环合得到嘧啶环,再经过锌粉还原、烷氧酰基化、甲基化反应得到利奥西呱(1),总收率12.4%(以14计)。
Ortho-Bromobenzyl (14) is condensed with hydrazine hydrate and then reacted with cyanopyruvic acid sodium salt (3) to obtain ethyl 5-amino-1- (2-fluorobenzyl) ), 4 and 1,1,3,3-tetramethoxypropane, and then through a series of functional group conversion reaction 1- (2-fluorobenzyl) -1H-pyrazolo [3,4-b] Pyridine-3-carboxamidine hydrochloride (9 ’), 9’ and benzeneazolidinonitrile (10) cyclization to give a pyrimidine ring, and then zinc reduction, alkoxylation, methylation reaction Osage (1), the total yield of 12.4% (in 14 dollars).