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Dibutyl 2-(trifluoromethyl)cyclopropylboronate as a useful (trifluoromethyl)cyclopropyl donor: application to antagonists of TRPV1
Tetrahedron Letters ( IF 1.5 ) Pub Date : 2009-12-21 , DOI: 10.1016/j.tetlet.2009.12.073
Matthew A.J. Duncton , Leticia Ayala , Carl Kaub , Satyanarayana Janagani , William T. Edwards , Nina Orike , Krithika Ramamoorthy , John Kincaid , Michael G. Kelly

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.



中文翻译:

2-(三氟甲基)环丙基硼酸二丁酯作为有用的(三氟甲基)环丙基供体:在TRPV1拮抗剂中的应用

可从市售试剂中一步获得的二丁基-2-(三氟甲基)环丙基硼酸酯2,通过参与钯催化的Suzuki偶联而用作有用的(三氟甲基)环丙基化试剂。通过制备TRPV1受体拮抗剂,举例说明了硼酸酯2在药物化学中的用途。

更新日期:2009-12-21
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