作者:Dennis Wetzl、Martin Gand、Alfred Ross、Hubertus Müller、Philipp Matzel、Steven P. Hanlon、Michael Müller、Beat Wirz、Matthias Höhne、Hans Iding
DOI:10.1002/cctc.201600384
日期:2016.6.21
Biocatalysis employing imine reductases is a promising approach for the one‐step generation of chiral amines from ketones. The enzymes reported for this process suffer from low activity and moderate stereoselectivity. We identified a set of enzymes that facilitate this reaction with high to quantitative conversions from a library of 28 imine reductases. This enabled the conversion of ketones with ammonia
使用亚胺还原酶的生物催化是一种从酮一步生成手性胺的有前途的方法。报道的用于该过程的酶具有低活性和适度的立体选择性。我们从28种亚胺还原酶的文库中鉴定出一组酶,可促进该反应的高转化率到定量转化率。这使得酮与氨,甲胺或丁胺的转化成为相应的胺。最重要的是,我们进行了制备性(> 100 mg)规模的胺合成,例如(1 S,3 R)-N,3-二甲基环己胺和(R)-N-甲基-2-氨基己烷,具有优异的立体化学纯度(98% de,96% ee),收益率很高。