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铜催化未活化的不饱和腙的烯键与多种羧酸的氨酰化反应,得到酯官能化的吡唑啉。

Cu-Catalyzed Aminoacyloxylation of Unactivated Alkenes of Unsaturated Hydrazones with Manifold Carboxylic Acids toward Ester-Functionalized Pyrazolines.

机构信息

State Key Laboratory of Applied Organic Chemistry, College of Chemistry and Chemical Engineering , Lanzhou University , Lanzhou , 730000 , PR China.

出版信息

Org Lett. 2018 Jul 20;20(14):4183-4186. doi: 10.1021/acs.orglett.8b01507. Epub 2018 Jul 6.

Abstract

A copper-catalyzed aminoacyloxylation of unactivated alkenes of unsaturated hydrazones is achieved by using various commercially available carboxylic acids as the acyloxylating reagents and di- tert-butyl peroxide (DTBP) as the oxidant. By using this method, a sequence of structurally diversiform acyloxyl-substituted pyrazolines are efficiently synthesized. Significantly, many carboxyl-containing drugs and bioactive molecules with unprotected functional groups are compatible in this reaction.

摘要

铜催化的未活化烯烃的氮杂羰氧基化反应通过使用各种商业上可用的羧酸作为酰氧基化试剂和二叔丁基过氧化物(DTBP)作为氧化剂来实现。通过使用这种方法,可以有效地合成一系列结构多样化的酰氧基取代的吡唑啉。值得注意的是,许多含有羧基的药物和具有未保护官能团的生物活性分子在这个反应中是相容的。

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