手性砌塊庫和合成模塊庫的構(gòu)建

楊立榮 吳堅(jiān)平 岑琦瓊

摘 要：成功構(gòu)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(gòu)建了5種新型酶-化學(xué)手性反應(yīng)模塊，例如脂肪酶拆分-Pd/LDH-DS消旋反應(yīng)模塊能夠在常溫下拆分芳香胺類，其中底物轉(zhuǎn)化率99%，產(chǎn)物ee值99%，突破生物拆分過程理論轉(zhuǎn)化率僅為50%的不足，過程的原子經(jīng)濟(jì)性與轉(zhuǎn)化效率較高，具有較大的創(chuàng)新性。

關(guān)鍵詞：手性砌塊 合成模塊 庫 化學(xué)-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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