对硝基氯苄经亚硫酸钠磺化、五氯化磷氯代、四氢吡咯取代、催化氢化、重氮化和还原制得4-(吡咯烷-1-基磺酰甲基)苯肼盐酸盐(7),与4-氯-1-羟基丁烷磺酸钠反应后,再经成腙、环合和甲基化“一锅法”制得阿莫曲坦粗品,经成富马酸盐纯化,再与苹果酸成盐制得苹果酸阿莫曲坦,总收率约6%(以对硝基氯苄计)。 P-Nitrobenzyl chloride was prepared by sulfonation with sodium sulfite, phosphorous chlorochloride, tetrahydropyrrole substitution, catalytic hydrogenation, diazotization and reduction to give 4- (pyrrolidin-1-ylsulfonylmethyl) phenylhydrazine hydrochloride Salt (7), with 4-chloro-1-hydroxy-butane sulfonate sodium reaction, and then by hydrazone, cyclization and methylation Acid salt purification, and then salt with malic acid in the manufacture of almotrigine malate, the total yield of about 6% (to nitrochlorobenzyl).