申请人:Taisho Pharmaceutical Co., Ltd.
公开号:EP2298755A1
公开(公告)日:2011-03-23
Production of a bicyclo[3.1.0]hexane derivative, useful as a metabotropic glutamate receptor modulator, becomes possible by a production method that includes converting a compound represented by Formula (II) into a compound represented by Formula (III) by reaction with an acyl group donor in the presence of a microorganism-derived enzyme, without using an expensive optically active trans hydroxy ester as a starting material and without employing a fluorination reaction requiring an ultralow temperature reaction. Furthermore, since asymmetric synthesis can be carried out in a stage closer to the final product, the production method is useful as a production method that can mass produce a bicyclo[3.1.0]hexane derivative.
生产双环[3.1.0]己烷衍生物可用作代谢型谷氨酸受体调节剂,其生产方法包括在微生物衍生酶存在下,通过与酰基供体反应,将式(II)代表的化合物转化为式(III)代表的化合物,而无需使用昂贵的光学活性反式羟基酯作为起始原料,也无需采用需要超低温反应的氟化反应。此外,由于不对称合成可在更接近最终产品的阶段进行,因此该生产方法可作为一种批量生产双环[3.1.0]己烷衍生物的生产方法。