AR-M390, ARM-390-药物合成数据库

【药物名称】AR-M390, ARM-390

化学结构式(Chemical Structure):

参考文献No.	37034
标题:	Novel cpds. with analgesic effect
作者:	Delorme, D.; Wei, Z.; Roberts, E. (AstraZeneca Canada Inc. ; AstraZeneca plc)
来源:	EP 0946511; US 6187792; WO 9828275

合成路线图解说明: 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No.	591936
标题:	A novel class of potent and exceptionally selective, nonpeptidic delta opioid receptor agonist
作者:	Brown, W.; et al.
来源:	16th Int Symp Med Chem (Sept 18 2000, Bologna) 2000,Abst PB-7

合成路线图解说明: 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.