公开(公告)号：EP2433942A1

公开(公告)日：2012-03-28

申请号：EP10777372.3

申请日：2010-05-20

申请人： Zhejiang Medicine Co., Ltd.

发明人： PAN, Yajin ,  PI, Shiqing ,  DING, Wenzhen ,  GU, Lixin ,  WEI, Angfeng ,  HE, Yimin

IPC分类号： C07D495/04 ,  C07D235/00 ,  C07D333/00

CPC分类号： C07D495/04

摘要： An Improved Preparation Method for D-Biotin
The invention discloses an improved preparation method for D-Biotin. If the composite method takes the diesteas the raw material, the finial biotin will be generated with impurities. The features of the invention refers to the improved preparation method for D-Biotin includes: firstly, (3aS,4S,6aR)-1,3-ωωω -butyl)-1 H -thiaphene[3,4-d]-2,4(1 H) -ketone is got after the methane tricarboxylic acid trialkyl ester and (3aR, 8aS, 8bS)-1,3-2-[3,4-d]thiophene [1,2-a]sulfuryl halide have the condensation reaction in the alkaline environment and then D-Biotin can be got after the reaction process of hydrolysis, decarbaxylation and closed loop. The invention succeeds in greatly improving the biotin quality from the original basis and simultaneously avoids the generation of impurities and the occurrence of side reaction.

摘要翻译： 一种改进的D-生物素制备方法本发明公开了一种改进的D-生物素制备方法。 如果复合方法将dieteas作为原料，最终的生物素会产生杂质。 本发明的特征是指改进的D-生物素制备方法，包括：首先，（3aS，4S，6aR）-1,3-ωωω-丁基）-1H-噻吩并[3,4-d] -2,4 （3aR，8aS，8bS）-1,3-2- [3,4-d]噻吩[1,2-a]硫酰卤进行缩合反应后得到（1H） - 酮 在碱性环境下进行水解反应，去羰基化和闭环反应后可得到D-生物素。 本发明成功地从原有基础上大幅度提高了生物素的质量，同时避免了杂质的产生和副反应的发生。