CRF_1受体阻滞剂类新型抗抑郁药DMP696的合成新方法  

New synthesis approach of the CRF_1 antagonist DMP696,an antidepressant

作　　者：梅德盛[1] 仲伯华[1] 

机构地区：[1]军事医学科学院毒物药物研究所,北京100850

出　　处：《中国新药杂志》2009年第1期70-72,共3页Chinese Journal of New Drugs

基　　金：国家"863"计划(2007AA02V400)

摘　　要：目的:合成促肾上腺皮质激素释放激素1(CRF1)受体阻滞剂类新型抗抑郁药DMP696。方法:以2,4-二氯苯乙腈为起始原料,经乙酰化、两次环化、氯代、偶联共5步合成DMP696。结果:目标化合物的总收率为10.5%,结构经1H-NMR、MS确证。结论:该方法合成路线短,试剂廉价易得,反应条件温和易控。Objective：To synthesize DMP696, a corticotropin-releasing factor 1 （CRF1 ） receptor antagonist with antidepressant activity. Methods： 2,4-Dichlorophenylaceonitrile was used as the starting material to synthesize DMP696 by 5 steps, i.e. acetylation, 2 steps of cyclocondensation, chlorination, and coupling. Results： The total yield was 10.5 % by the process. The structure was confirmed by ^1H-NMR and MS. Conclusion： The reagents in this approach are cheaper, and the reaction condition is easy to control. The route is a new synthesis approach of DMP696.

关 键 词：DMP696 促肾上腺皮质激素释放激素1(CRF1 )受体阻滞剂 抗抑郁药 药物合成 

分 类 号：R971.43[医药卫生—药品] R916.41[医药卫生—药学]