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YM-44778(fumarate salt (1:1))

N-[2-(3,4-二氯苯基)-4-[3-氧基-1,2,3,4-四氢螺蓄[异喹啉-1,4'-哌啶]-1'-基]丁基]-3,4,5-三甲氧基-N-甲基苯甲酰Chemical Name: N-[2-(3,4-Dichlorophenyl)-4-[3-oxo-1,2,3,4-tetrahydrospiro[isoquinoline-1,4'-piperidin]-1'-yl]butyl]-3,4,5-trimethoxy-N-methylbenzamide
CAS No. 173941-74-7, 173941-75-8 (fumarate(1:1))
项目整合开发状态: Biological Testing
项目研究机构: Yamanouchi (Originator)
合成路线: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: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.
📌 参考资料/链接:
参考文献标题: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
文献作者:Kubota,H.; Kakefuda,A.; Okamoto,Y.; Fujii,M.; Yamamoto,O.; Yamagiwa,Y.; Orita,M.; Ikeda,K.; Takeuchi,M.; Shibanuma,T.; Isomura,Y.
参考来源:Chem Pharm Bull 1998,46(10),1538

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产品链接: CAS No. 173941-74-7››