| 新型酰基供体用于酶法动力学拆分制备(R)-1-(2-萘基)乙胺的研究 |
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| 引用本文： | 符思敏,徐刚,陈永军,吴坚平,杨立荣.新型酰基供体用于酶法动力学拆分制备(R)-1-(2-萘基)乙胺的研究[J].有机化学,2012,32(3):526-531. |
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| 作者姓名： | 符思敏 徐刚 陈永军 吴坚平 杨立荣 |
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| 作者单位： | 浙江大学化学工程与生物工程学系 杭州310027 |
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| 基金项目： | 国家自然科学基金(Nos.20606030,20936002);国家863计划(No.2006AA02Z238);国家973计划(Nos.2011CB710800,2009CB724706)资助项目~~ |
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| 摘 要： | 首次成功实现了光学纯(R)-1-(2-萘基)乙胺的高效酶法动力学拆分制备,考察了脂肪酶种类、溶剂、酰基供体、底物浓度、反应温度等对拆分效果的影响,发现新型酰基供体——正戊酸对氯苯酯能够很好地抑制非酶促自催化酰胺化效应.在甲苯溶剂中,底物浓度300 mmol/L,40℃条件下,采用该供体在脂肪酶Novozym 435催化下,动力学拆分反应8 h转化率达到理论最佳值50%,eep>99%.
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| 关 键 词： | (R)-1-(2-萘基)乙胺 正戊酸对氯苯酯 Novozym 435 酶动力学拆分 |
Preparation of (R)-1-(2-Naphthyl)ethylamine by Enzymatic Kinetic Resolution with A New Acyl Donor |
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| Fu, Simin
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Xu, Gang
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Chen, Yongjun
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Wu, Jianping
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Yang, Lirong.Preparation of (R)-1-(2-Naphthyl)ethylamine by Enzymatic Kinetic Resolution with A New Acyl Donor[J].Chinese Journal of Organic Chemistry,2012,32(3):526-531. |
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| Authors: | Fu Simin Xu Gang Chen Yongjun Wu Jianping Yang Lirong |
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| Institution: | Fu,Simin Xu,Gang Chen,Yongjun Wu,Jianping Yang,Lirong(Department of Chemical and Biological Engineering,Zhejiang University,Hangzhou 310027) |
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| Abstract: | Enantiomerically pure(R)-1-(2-naphthyl)ethylamine was firstly prepared by an efficient enzymatic kinetic resolution process.The effects of lipases,solvents,acyl donors,substrate concentration and temperature on the reaction were investigated.It was found that as the acyl donor,4-chlorophenyl valerate could effectively inhibit the non-selective amidation reaction.The optimal solvent,amine concentration and temperature were toluene,300 mmol/L and 40 ℃,respectively.Under the optimal conditions mentioned above,an excellent eepvalue(>99%) at high conversion(50%) in 8 h could be achieved on the kinetic resolution reaction catalyzed by Novozym 435 with the new acyl donor. |
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| Keywords: | (R)-1-(2-naphthyl) ethylamine 4-chlorophenyl valerate Novozym 435 enzymatic kinetic resolution |
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