手性砌块库和合成模块库的构建

杨立荣 吴坚平 岑琦琼

摘 要：成功构建了包括新型卤代醇、羟基氰、芳香醇、脂肪醇和芳香胺的手性砌块库，涵盖108种手性化合物。构建了5种新型酶-化学手性反应模块，例如脂肪酶拆分-Pd/LDH-DS消旋反应模块能够在常温下拆分芳香胺类，其中底物转化率99%，产物ee值99%，突破生物拆分过程理论转化率仅为50%的不足，过程的原子经济性与转化效率较高，具有较大的创新性。

关键词：手性砌块 合成模块 库 化学-酶法 脂肪酶 拆分

Abstract：A chiral block library， including 108 kinds of chiral chemicals， were constructed. 5 types of novel chem-enzymatic synthesis modules were also developed. For example， the module of lipase coupled with Pd/LDH-DS was successfully used in the resolution of aromatic amine with the excellent results of conversion of 99% and eep of 99%. The atom economy and conversion efficiency were greatly improved with this novel module.

Key Words：Chiral block；Synthesis module；Library；Chem-enzymatic method；Lipase；resolution

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