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一个成功的d-生物素(1)合成法必须克服分子中三个相邻不对称中心所带来的关键性障碍。作者试图将一个带有受掩蔽的α-氨基又有特定几何形状的烯醇酯,与有适当取代的带生物素戊酸侧链的亚胺加成,以建立生物素必需的立体化学特点。并试图将醇醛缩合的资料应用于亚胺化学。
A successful synthesis of d-biotin (1) must overcome the critical obstacles posed by three adjacent asymmetric centers in the molecule. The authors attempted to incorporate an enolase ester with a masked alpha-amino group and a specific geometry with an appropriately substituted imide with a biotin valerate side chain to establish the necessary stereochemical features of biotin. And tried to apply aldol condensation to imine chemistry.