A Synthesis of 1H-Indazoles via a Cu(OAc)2-Catalyzed N-N Bond Formation

被引：63

作者：

Chen, Cheng-yi ^{[1
]}

Tang, Guangrong ^{[2
]}

He, Fengxian ^{[2
]}

Wang, Zhaobin ^{[2
]}

Jing, Hailin ^{[2
]}

Faessler, Roger ^{[1
]}

机构：

[1] Cilag AG, Small Mol API Switzerland, Pharmaceut Dev & Mfg Sci, Janssen R&D, Hochstr 201, CH-8205 Schaffhausen, Switzerland

[2] Porton Shanghai R&D Ctr, 1299 Ziyue Rd,Zizhu Sci Pk, Shanghai 200241, Peoples R China

来源：

ORGANIC LETTERS | 2016年 / 18卷 / 07期

关键词：

INDAZOLE-TYPE ALKALOIDS; ONE-POT SYNTHESIS; EFFICIENT SYNTHESIS; NIGELLA-SATIVA; H AMIDATION; IN-VITRO; DERIVATIVES; BENZYDAMINE; SEEDS; FUNCTIONALIZATION;

D O I：

10.1021/acs.orglett.6b00611

中图分类号：

O62 [有机化学];

学科分类号：

070303 ; 081704 ;

摘要：

A facile synthesis of 1H-indazoles featuring a Cu(OAc)(2)-catalyzed N-N bond formation using oxygen as the terminal oxidant is described. The reaction of readily available 2-aminobenzonitriles with various organometallic reagents led to o-aminoaryl N-H ketimine species. The subsequent Cu(OAc)(2)-catalyzed N-N bond formation in DMSO under oxygen afforded a wide variety of 1H-indazoles in good to excellent yields.

引用

页码：1690 / 1693

页数：4

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