[Problem] A compound which can be used as a pharmaceutical, particularly a insulin secretion promoter or a agent for preventing/treating disease in which GPR40 is concerned such as diabetes or the like, is provided.
[Means for resolution] It was found that an oxadiazolidinedione compound which is characterized by the possession of a benzyl or the like substituent binding to the cyclic group via a linker at the 2-position of the oxadiazolidinedione ring, or a pharmaceutically acceptable salt thereof, has excellent GPR40 agonist action. In addition, since the oxadiazolidinedione compound of the present invention showed excellent insulin secretion promoting action and blood glucose level-lowering action, it is useful as an insulin secretion promoter or an agent for preventing/treating diabetes.
[EN] BENZO PIPERIDINE RING AND BENZO MORPHOLINE RING COMPOUNDS, MANUFACTURING METHOD THEREFOR, AND MEDICAL APPLICATIONS THEREOF<br/>[FR] COMPOSÉS DE CYCLE BENZOPIPÉRIDINE ET DE CYCLE BENZOMORPHOLINE, PROCÉDÉ DE PRÉPARATION ET APPLICATIONS MÉDICALES DE CES COMPOSÉS
A New Family of Tunable Indolylphosphine Ligands by One-Pot Assembly and Their Applications in Suzuki−Miyaura Coupling of Aryl Chlorides
作者:Chau Ming So、Chung Chiu Yeung、Chak Po Lau、Fuk Yee Kwong
DOI:10.1021/jo801544w
日期:2008.10.3
This study describes a new class of indolylphosphine ligands, which can be easily accessed by a simple one-pot assembly from commercially available indoles, acid chlorides, and chlorophosphines. A combination of these three starting materials provides a high diversification of the ligand structure. The application of this ligand array in palladium-catalyzed Suzuki-Miyaura coupling reaction of aryl chlorides with arylboronic acids is described. A catalyst loading down to 0.01 mol % of Pd can be achieved.