科研之友
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摘要
Enantio- and diastereoselective one-pot synthesis of three- to seven-membered cis-azaheterocycles was achieved using a triggered asymmetric conjugate addition reaction of lithium amide with an enoate, followed by C- and N-alkylation of the resulting lithium 3-aminoenolate with alpha, omega-dihaloalkane, which can be regarded as a [1+2+n] cyclization. The usefulness of the developed methodology was clearly demonstrated by the short-step asymmetric syntheses of azirinomycin ester, nemonapride, and kopsinine.
- 出版日期2013-9
