手性三氯乙酰亚胺酯的钯催化环化反应合成 1,3-氨基醇。
Stereoselective synthesis of 1,3-amino alcohols by the Pd-catalyzed cyclization of trichloroacetimidates.
出版信息
J Org Chem. 2014 Feb 7;79(3):1289-1302. doi: 10.1021/jo402681z.
PMID:24422508
Abstract
The synthesis of 4-vinyl-5,6-dihydro-1,3-oxazines, precursors of 1,3-amino alcohols, using the palladium-catalyzed cyclization of trichloroacetimidates is reported. The reaction favors the formation of the 4,6-cis-isomers with up to >20:1 diastereoselectivity. Chemoselective hydrolysis of the resulting 5,6-dihydro-1,3-oxazines was also investigated.
摘要
报告了使用钯催化三氯乙酰胺的环化反应合成 4-乙烯基-5,6-二氢-1,3-恶嗪，这是 1,3-氨基醇的前体。该反应有利于形成高达 >20:1 非对映选择性的 4,6-顺式异构体。还研究了所得 5,6-二氢-1,3-恶嗪的选择性水解。
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