YM-44778(fumarate salt (1:1))-药物合成数据库

【药物名称】YM-44778(fumarate salt (1:1))

化学结构式(Chemical Structure):

参考文献No.	476999
标题:	Spiro-substituted piperidines as neurokinin receptor antagonists. III. Synthesis of (?-N-[2-(3,4-dichlorophenyl)-4-(spiro-substituted piperidin-1'-yl)butyl]-N-methylbenzamides and evaluation of NK1-NK2 dual antagonistic activities
作者:	Kubota, H.; Kakefuda, A.; Okamoto, Y.; Fujii, M.; Yamamoto, O.; Yamagiwa, Y.; Orita, M.; Ikeda, K.; Takeuchi, M.; Shibanuma, T.; Isomura, Y.
来源:	Chem Pharm Bull 1998,46(10),1538

合成路线图解说明: The cyclization of cyanogen chloride (I) with aqueus methylamine (II) at 150 C in a pressure vessel gives N2,N4,N6-trimethylmelamine (III), which is then treated with aqueous formaldehyde at pH 8.9.

合成路线图解说明: Treatment of alcohol (I) with methanesulfonyl chloride in the presence of triethylamine provided mesylate (II), which was condensed with the spirosubstituted piperidine (III) to give the desired compound.