Tian Shi-Kai, Hong Ran, Deng Li
Department of Chemistry, Brandeis University, Waltham, MA 02454-9110, USA.
J Am Chem Soc. 2003 Aug 20;125(33):9900-1. doi: 10.1021/ja036222p.
The development of broadly applicable and practical catalytic approaches for the enantioselective creation of quaternary stereocenters remains a highly desirable yet challenging goal. In this Communication, we describe a highly enantioselective cyanosilylation of acetal ketones (alpha,alpha-dialkoxy ketones) catalyzed by modified cinchona alkaloids. This reaction is the first highly enantioselective cyanosilylation of ketones catalyzed by an organic chiral Lewis base and is found to be highly efficient with acetal ketones bearing a broad range of alkyl, aryl, alkenyl, and alkynyl substituents. This new catalytic asymmetric reaction, coupled with the versatility of the acetal functionality, provides a broadly useful synthetic method for chiral building blocks bearing quaternary stereocenters. Acetal ketones, readily accessible but previously unexplored in asymmetric synthesis, demonstrate unusual reactivity and selectivity toward the nucleophilic cyanosilylation, thereby suggesting that they may be interesting substrates for other catalytic enantioselective reactions.
开发用于对映选择性构建季碳立体中心的广泛适用且实用的催化方法仍然是一个极有吸引力但具有挑战性的目标。在本通讯中,我们描述了一种由修饰的金鸡纳生物碱催化的缩酮(α,α-二烷氧基酮)的高度对映选择性氰基硅烷化反应。该反应是有机手性路易斯碱催化的首例酮的高度对映选择性氰基硅烷化反应,并且发现对于带有广泛烷基、芳基、烯基和炔基取代基的缩酮具有高效性。这种新的催化不对称反应,结合缩酮官能团的多功能性,为带有季碳立体中心的手性结构单元提供了一种广泛有用的合成方法。缩酮易于获得,但此前在不对称合成中未被探索,其对亲核氰基硅烷化表现出异常的反应性和选择性,从而表明它们可能是其他催化对映选择性反应的有趣底物。