Palladium-catalyzed Suzuki cross-coupling of aryl halides with aryl boronic acids in the presence of glucosamine-based phosphines
摘要:
Carbohydrate-substituted phosphines are easily obtained in quite good yields by coupling of protected or non-protected D-glucosamine with the corresponding diphenylphosphino acid. These neutral ligands, in association with palladium acetate, are very active catalysts in the Suzuki cross-coupling reaction. The polyhydroxy phosphines are more active than the peracetylated phosphines. The process tolerates electron-rich as well as electron-poor substituents. Excellent turnovers, up to 97 000 are observed. (C) 2003 Elsevier Science B.V. All rights reserved.
[EN] CARBOXAMIDE DERIVATIVES AS ION CHANNEL MODULATORS<br/>[FR] DERIVES DE CARBOXAMIDE UTILISES EN TANT QUE MODULATEURS DES CANAUX IONIQUES
申请人:WYETH CORP
公开号:WO2008073936A1
公开(公告)日:2008-06-19
[EN] The present teachings provide compounds of Formula (I) wherein Ar, R1, R2, R3, X, p and n are defined herein. The present teachings also provide processes for producing said compounds and methods of treating a pathological condition or disorder, or alleviating a symptom thereof, using said compounds. The compounds can be useful in modulating ion channel activity including treating a variety of conditions associated with the abnormal modulation of one or more voltage-gated calcium channels. [FR] L'invention concerne des composés de Formule (I) dans laquelle Ar, R1, R2, R3, X, p et n sont tels que définis dans la description. L'invention concerne également des procédés de production de ces composés ainsi que des méthodes de traitement d'une affection ou d'un trouble pathologique, ou d'atténuation d'un symptôme associé, au moyen desdits composés. Les composés selon l'invention peuvent être utiles dans la modulation de l'activité des canaux ioniques, notamment dans le traitement de diverses affections associées à la modulation anormale d'au moins un canal calcique sensible au voltage.
WO2008/73461
申请人:——
公开号:——
公开(公告)日:——
Palladium-catalyzed Suzuki cross-coupling of aryl halides with aryl boronic acids in the presence of glucosamine-based phosphines
Carbohydrate-substituted phosphines are easily obtained in quite good yields by coupling of protected or non-protected D-glucosamine with the corresponding diphenylphosphino acid. These neutral ligands, in association with palladium acetate, are very active catalysts in the Suzuki cross-coupling reaction. The polyhydroxy phosphines are more active than the peracetylated phosphines. The process tolerates electron-rich as well as electron-poor substituents. Excellent turnovers, up to 97 000 are observed. (C) 2003 Elsevier Science B.V. All rights reserved.