Solid-phase synthesis of skeletally diverse benzofused sultams via palladium-catalyzed cyclization

Solid-phase synthesis of skeletally diverse benzofused sultams via palladium-catalyzed cyclization
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通过钯催化环化固相合成骨架多样的苯并稠合磺内酯

DOI:
10.1016/j.tetlet.2011.01.055
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发表时间:
2011-03-30
影响因子:
1.8
通讯作者:
Yu, Yongping
Yu, Yongping
中科院分区:
化学4区
文献类型:
--
作者:
Chen, Wenteng;Li, Zhi;Yu, Yongping

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本文介绍了由树脂结合的氨基酸固相合成磺内酰胺的方法。与树脂结合的伯胺的磺酰化得到所需的仲胺,之后分子内Buchwald-Hartwig型偶联形成C-S键。磺酰胺上的最终烷基化随后裂解提供相应的七元磺内酰胺。(c)2011爱思唯尔有限公司保留所有权利。
The solid-phase synthesis of sultams from resin-bound amino acids is described. The sulfonylation of the resin-bound primary amines afforded the requisite secondary amines, after which the intramolecular Buchwald-Hartwig-type coupling forms the C-S bond. A final alkylation on the sulfonamides followed by cleavage provided the corresponding seven-membered sultams. (c) 2011 Elsevier Ltd. All rights reserved.