| 摘要 |
PURPOSE: To readily obtain the subject compound, especially cis isomer useful as an intermediate for medicines in good conversion and yield by subjecting a cyclopropenecarboxylic acid derivative to asymmetric hydrogenation in the presence of a specific metal catalyst. CONSTITUTION: This method for producing a compound of the formula II is to subject a cyclopropenecarboxylic acid derivative of formula I (R<1> is a lower alkyl, a 5-8C cycloalkyl, an aryl or a 5-6C heterocycle; R<2> is H, a lower alkyl or an aryl) to asymmetric hydrogenation in the presence of (B) a metal catalyst (e.g. metal component is a metal catalyst of Rh, Ir or Ru) modified with an optically active metallocenylphosphine derivative of formula II [R<3> and R<4> are each a lower alkyl; R<5> and R<6> are each H, lower alkyl, etc.; Ph is phenyl; M is Fe or Ru; (n) is 1-3]. The reaction is normally carried out in an organic solvent such as methanol and hydrogen pressure in reduction is ordinary pressure to 500kg/cm<2> and when a tert. amine such as triethylamine is added to the reaction system, the reactivity is improved. |
