申请人:Matsumoto Yoshinori
公开号:US20090043110A1
公开(公告)日:2009-02-12
The present invention is to provide a novel method for producing (2S)-2-benzyl-3-(cis-hexahydro-2-isoindolinylcarbonyl)propionic acid which is useful as a therapeutic agent for diabetes. The present invention relates to a method for producing (2S)-2-benzyl-3-(cis-hexahydro-2-isoindolinylcarbonyl)propionic acid, which is characterized in that 2-benzylidene-3-(cis-hexahydro-2-isoindolinylcarbonyl)propionic acid is subjected to a catalytic reduction reaction in the presence of an asymmetric catalyst prepared from a pyrrolidinebisphosphine compound (I) represented by the following general formula (I):
wherein, R
1
represents a linear or branched alkyl group having 1-10 carbon atoms, cycloalkyl group, aralkyl group or aryl group which may respectively have a substituent; and R
2
and R
3
independently represent an optionally substituted aryl group. The * mark in the pyrrolidine ring shows that the carbon atom at that position has the S configuration, and a rhodium compound.
本发明旨在提供一种新的制备(2S)-2-苄基-3-(顺式-六氢-2-异吲哚基甲酰)丙酸的方法,该方法可用作糖尿病治疗剂。本发明涉及一种制备(2S)-2-苄基-3-(顺式-六氢-2-异吲哚基甲酰)丙酸的方法,其特征在于将2-苄基亚甲基-3-(顺式-六氢-2-异吲哚基甲酰)丙酸在不对称催化剂的存在下进行催化还原反应,该不对称催化剂由下式(I)表示的吡咯烷双膦化合物制备而成:其中,R1代表具有1-10个碳原子的线性或支链烷基、环烷基、芳基烷基或芳基,它们可以分别具有取代基;R2和R3独立地代表可选取代的芳基。吡咯烷环中的*标记表示该位置的碳原子具有S构型,还包括一种铑化合物。