公开(公告)号：US20120065406A1

公开(公告)日：2012-03-15

申请号：US13321606

申请日：2010-05-20

申请人： Yajin Pan ,  Shiqing Pi ,  Wenzhen Ding ,  Lixin Gu ,  Angfeng Wei ,  Yimin He

发明人： Yajin Pan ,  Shiqing Pi ,  Wenzhen Ding ,  Lixin Gu ,  Angfeng Wei ,  Yimin He

IPC分类号： C07D495/04

CPC分类号： C07D495/04

摘要： The invention discloses the improved preparation method for D-Biotin. If the composite method takes the malonic acid diester as 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-dibenzyl-4-(ω,ω,ω-3 -alkoxycarbonyl bytyl)-4H-1H-thiophene[3,4-d]iminazole-2,4(1H)-ketone is got after the methane tricarboxylic acid trialkyl ester and (3aR,8aS,8bS)-1,3-dibenzyl-2-oxo-10H-iminazole[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, decarboxylation 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： 本发明公开了改进的D-生物素制备方法。 如果复合方法以丙二酸二酯为原料，则会使杂质生成最终生物素。 本发明的特征是改进的D-生物素的制备方法，包括：首先，（3aS，4S，6aR）-1,3-二苄基-4-（ω，ω，ω-3-烷氧基羰基） 在甲烷三羧酸三烷基酯和（3aR，8aS，8bS）-1,3-二苄基-2-氧代-10H-哒嗪酮后得到1H-噻吩[3,4-d]亚氨基-1,2（1H） - 酮 亚胺唑[3,4-d]噻吩[1,2-a]磺酰卤在碱性环境中具有缩合反应，然后在水解，脱羧和闭环反应过程后得到D-生物素。 本发明成功地从原始基础上大大提高了生物素质量，同时避免了杂质的产生和副反应的发生。