AR-M390, ARM-390
N,N-二乙基-4-[1-苯基-1-(4-吡哌啶基苯)甲基]苯扎米Chemical Name: N,N-Diethyl-4-[1-phenyl-1-(4-piperidinylidene)methyl]benzamide
CAS No. 209808-01-5, 209808-47-9 (monohydrochloride)
项目整合开发状态: Preclinical
项目研究机构: AstraZeneca (Originator)
合成路线:4-Benzoylpiperidine (I) was converted to the N-Boc derivative (II) by treatment with Boc2O in the presence of Na2CO3.4-Iodo-N,N-diethylbenzamide (III) was subjected to metal-halogen exchange with tert-butyllithium,and the resulting organolithium derivative (IV) was condensed with ketone (II) to give carbinol (V).Finally,dehydration of the benzhydryl alcohol of (V) with concomitant N-Boc group cleavage in the presence of trifluoroacetic acid furnished the title compound.
📌 参考资料/链接：
参考文献标题:Novel cpds.with analgesic effect
文献作者:Delorme,D.; Wei,Z.; Roberts,E.(AstraZeneca Canada Inc.; AstraZeneca plc)
参考来源:EP 0946511; US 6187792; WO 9828275
📄 详细内容
合成路线:4-Benzoylpiperidine (I) was converted to the N-Boc derivative (II) by treatment with Boc2O in the presence of Na2CO3.4-Iodo-N,N-diethylbenzamide (III) was subjected to metal-halogen exchange with tert-butyllithium,and the resulting organolithium derivative (IV) was condensed with ketone (II) to give carbinol (V).Finally,dehydration of the benzhydryl alcohol of (V) with concomitant N-Boc group cleavage in the presence of trifluoroacetic acid furnished the title compound.
参考文献标题:A novel class of potent and exceptionally selective,nonpeptidic delta opioid receptor agonist
文献作者:Brown,W.; et al.
参考来源:16th Int Symp Med Chem (Sept 18 2000,Bologna) 2000,Abst PB-7
产品链接: CAS No. 209808-01-5›› 产品链接: CAS No.209808-47-9››