Dibutyl 2-(trifluoromethyl)cyclopropylboronate as a useful (trifluoromethyl)cyclopropyl donor: application to antagonists of TRPV1

被引：35

作者：

Duncton, Matthew A. J. ^{[1
]}

Ayala, Leticia ^{[1
]}

Kaub, Carl ^{[1
]}

Janagani, Satyanarayana ^{[1
]}

Edwards, William T. ^{[1
]}

Orike, Nina ^{[1
]}

Ramamoorthy, Krithika ^{[1
]}

Kincaid, John ^{[1
]}

Kelly, Michael G. ^{[1
]}

机构：

[1] Renovis Inc, San Francisco, CA 94080 USA

来源：

TETRAHEDRON LETTERS | 2010年 / 51卷 / 07期

关键词：

STEREOSELECTIVE-SYNTHESIS; CYCLOPROPYLBORONIC ACID; PRIVILEGED STRUCTURES; N-CYCLOPROPYLATION; CARBENE TRANSFER; CYCLOPROPANE; FLUORINE; RECEPTOR; AMIDES; PAIN;

D O I：

10.1016/j.tetlet.2009.12.073

中图分类号：

O62 [有机化学];

学科分类号：

070303 [有机化学];

摘要：

Dibutyl-2-(trifluoromethyl)cyclopropylboronate 2, available in one step from commercially available reagents, serves as a useful (trifluoromethyl)cyclopropylating reagent by participating in a palladium-catalyzed Suzuki coupling. The use of boronate ester 2 in medicinal chemistry was exemplified by preparation of TRPV1 receptor antagonists. (C) 2009 Elsevier Ltd. All rights reserved.

引用

页码：1009 / 1011

页数：3

共 46 条

[1]

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[2]

[Anonymous], 2006, CHAPTER 3PRIVILEGED

[3]

REACTION OF TRIFLUOROMETHYLCARBENE WITH CIS- AND TRANS-BUT-2-ENES [J].