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自Goldkrg&Sternbach首次合成d—生物素后,在图1中,哪一种是所需结构,多年来已经在技术上得到很好证明。与其它已公开发表的合成方法进行比较后,其主要优势在于立体专一性。一方面当原材料和相应的2羧酸依丁迪咪唑被拆分后,通过对反丁烯二酸的选择,在化合物4和5中依丁咪唑环上C原子的构型得到保持;另一方面在噻嗯酮3,4—d咪唑三环侧链的连接点通过5个中间产物立体定向的氢化作用,相关的构型也被确定。
After the first synthesis of d-biotin by Goldkrg & Sternbach, which one is the desired structure in Figure 1 has been technically well documented over the years. Compared with other published methods of synthesis, its main advantage lies in three-dimensional specificity. On the one hand, after the starting material and the corresponding dicididazole are resolved, the choice of fumaric acid is maintained in the C atom configuration of the ethephon ring in compounds 4 and 5; on the other hand, In the tetramethylthiazolone 3,4-d imidazole tricyclic side chain point of attachment through the intermediates of 5 stereospecific hydrogenation, the associated configuration is also determined.