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Chemoenzymatic Preparation of 1??Heteroarylethanamines of Low Solubility

J Brem, LC Bencze, A Liljeblad…

文献索引:Brem, Juergen; Bencze, Laszlo-Csaba; Liljeblad, Arto; Turcu, Mihaela C.; Paizs, Csaba; Irimie, Florin-Dan; Kanerva, Liisa T. European Journal of Organic Chemistry, 2012 , # 17 p. 3288 - 3294

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被引用次数: 7

摘要

Abstract Both enantiomers of biologically and pharmaceutically interesting benzofuran-, benzothiophen-, and phenylfuran-based 1-heteroarylethanamines were prepared at close to theoretical yields by using Candida antarctica lipase B (Novozym 435) catalyzed (R)- selective N-acylation with isopropyl butanoate (enantiomeric ratio E> 200). The use of N- methyl-2-pyrrolidinone (NMP) as a cosolvent (1: 30) in isopropyl butanoate solved the ...