发明名称 PROCESS FOR THE PREPARATION OF ARYLETHANOLAMINE DERIVATIVES HAVING AN ANTI-OBESITY AND ANTI-DIABETIC PROPERTIES
摘要 A process for the preparation of a compound of Formula (IA) or a pharmaceutically acceptable salt thereof: wherein R1 is an aryl, pyridyl, thiazolyl, phenoxymethyl, or pyrimidyl group, optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxy, C1 - 6alkoxy, C1-6alkyl, hydroxymethyl, trifluoromethyl, -NR6R6, and -NHSO2R6, where each R6 is independently hydrogen or C1-4alkyl; R2 is hydrogen or C1- 6alkyl; R3 is CO2R7 where R7 is hydrogen or C1-6alkyl; R4 and R5 are independently hydrogen, C1-6alkyl, or -CO2C1-6alkyl; and Y is N or CH comprising the step of preparing a diamide of Formula (II) or a pharmaceutically acceptable salt thereof: wherein R1 is an aryl, pyridyl, thiazolyl, phenoxymethyl, or pyrimidyl group, optionally substituted by one or more substituents selected from the group consisting of halogen, hydroxy, C1 - 6alkoxy, C1-6alkyl, hydroxymethyl, trifluoromethyl, -NR6R6, and -NHSO2R6, where each R6 is independently hydrogen or C1-4alkyl; R2 is hydrogen or C1- 6alkyl; R3 is CO2R7 where R7 is C1-6alkyl; R4 and R5 are independently hydrogen, C1-6alkyl, -CO2C1-6alkyl; and Y is N or CH.
申请公布号 CA2394117(A1) 申请公布日期 2001.06.14
申请号 CA20002394117 申请日期 2000.12.08
申请人 GLAXO GROUP LIMITED 发明人 LAWRENCE, RONNIE MAXWELL;MILLAR, ALAN
分类号 C07D213/803;C07B61/00;C07C209/36;C07C209/58;C07C213/02;C07C215/14;C07C229/52;C07C231/02;C07C237/04;C07C237/06;C07C237/22;C07D213/38;C07D213/40;(IPC1-7):C07C237/06;A61P3/04;A61P3/10;A61K31/24;A61K31/44;C07D213/80 主分类号 C07D213/803
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