通过使用手性Ru(II)催化剂和HCO 2 H / Et 3 N的共沸溶液作为氢供体,通过动态动力学拆分,开发了β-酮磺酰胺的高度对映选择性转移加氢反应,可提供良好的α-取代的β-羟基磺酰胺产生具有优异的非对映选择性和对映选择性的产物。该方法具有条件温和,操作简便,底物范围广的特点,可以在合成天然产物和含有α-取代的β-羟基磺酰胺核心的生物活性化合物中找到广泛的应用。
Synthesis and reactivity of N-alkyl-2-oxoalkanesulfonamides
作者:Juan A. Vega、Ramón Alajarín、Juan J. Vaquero、Julio Alvarez-Builla
DOI:10.1016/s0040-4020(98)00093-3
日期:1998.4
A series of N-alkyl-2-oxoalkanesulfonamides have been synthesized by reacting silyl enol ethers with N-alkyl-sulfamoyl chlorides. Their reactivity towards electrophiles was investigated in order to explore the regio-and stereoselectivity of the process. 2-Oxoalkanesulfonamides were used to prepare 5-(methylsulfamoyl)-1,4-dihydropyridines derivatives. (C) 1998 Elsevier Science Ltd. All rights reserved.