【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
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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%.
For the first time, the preparation of optically pure (R) -1- (2-naphthyl) ethylamine by enzymatic kinetic resolution was successfully carried out. The effects of lipase type, solvent, acyl donor, substrate concentration and reaction temperature The results showed that the new acyl donor-p-chlorophenyl p-valerate could inhibit the non-enzymatic self-catalytic amidation effectively.Under the conditions of toluene concentration of 300 mmol / L and 40 ℃ Under the catalytic condition of Novozym 435 lipase, the conversion efficiency of the donor reached 50% of the theoretical optimum value and eep> 99% after 8 h of kinetic resolution.
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