手性砌塊庫和合成模塊庫的構建

楊立榮 吳堅平 岑琦

摘 要：成功構建了包括新型鹵代醇、羥基氰、芳香醇、脂肪醇和芳香胺的手性砌塊庫，涵蓋108種手性化合物。構建了5種新型酶-化學手性反應模塊，例如脂肪酶拆分-Pd/LDH-DS消旋反應模塊能夠在常溫下拆分芳香胺類，其中底物轉化率99%，產物ee值99%，突破生物拆分過程理論轉化率僅為50%的不足，過程的原子經濟性與轉化效率較高，具有較大的創新性。

關鍵詞：手性砌塊 合成模塊 庫 化學-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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