Highly Enantioselective Direct Asymmetric Reductive Amination of 2-Acetyl-6-Substituted Pyridines
作者:Masatoshi Yamada、Kazuki Azuma、Mitsuhisa Yamano
DOI:10.1021/acs.orglett.1c00848
日期:2021.5.7
direct asymmetric reductive amination of a variety of ketone substrates, including 2-acetyl-6-substituted pyridines, β-keto esters, β-keto amides, and 1-(6-methylpyridin-2-yl)propan-2-one, has been disclosed for the first time (94.6% to >99.9% ee). With ammonium trifluoroacetate as the nitrogen source, various chiral corresponding primary amines were prepared in excellent enantioselectivity and conversion
多种酮类底物的高度直接不对称还原胺化反应,包括2-乙酰基-6-取代的吡啶,β-酮基酯,β-酮基酰胺和1-(6-甲基吡啶-2-基)丙-2-酮首次公开(ee为94.6%至> 99.9%)。以三氟乙酸铵为氮源,在市售廉价的手性催化剂Ru(OAc)2 (S)-binap}存在下,在0.8 MPa的氢气压力下,以优异的对映选择性和转化率制备了各种手性的相应伯胺。气压。