To produce the subject compound in excellent yield on an industrial scale according to an uncomplicated method by passing a specific vinyl compound through a reaction with a specified carbene.
(A) An N vinyl compound represented by formula I (R1 to R3 are each H, a 1-6C alkyl, a halogen, a 1-6C halogenoalkyl or a 1-6C alkoxy; R4 is H, a 1-6C alkyl or a 6-12C aryl; Y is an open-chain or a cyclic 1-12C alkoxy, a 6-12C aryl, a 7-12C aralkyl, a 7-12C aralkyloxy or an open-chain or a cyclic 1-12C alkyl) is reacted with (B) a carbene represented by the formula FXC (X is Cl or Br) to provide a cyclopropylamine derivative represented by formula II. The X in the derivative represented by formula II is then substituted with H by reduction and COY group and (un)substituted benzyl group are finally eliminated from the N to prepare the objective compound. For example, N- benzyl-N-(2-chloro-2-fluorocyclopropyl)-benzylcarbamate is preferably used as the derivative represented by formula II.
ARUBUREHITO MARUHOORUTO
SHIYUTEFUAN BEEMU
