NIP-530
Chemical Name: N'-[3,5-Bis(trifluoromethyl)benzyl]-N-[3-[N-[1-(4-fluorobenzyl)benzimidazol-2-yl]-N-methylamino]propyl]-N-methylurea hydrochloride
CAS No. 215583-22-5
项目整合开发状态: Preclinical
项目研究机构: Nissan Chemical (Originator)
合成路线:The reaction of 2-chlorobenzimidazole (I) with N,N'-dimethylprolylene-1,3-diamine (II) by heating at 130 C gives N-(1H-benzimidazol-2-yl)-N,N'-dimethylpropylene-1,3-diamine (III),which is treated with tert-butoxycarbonyl anhydride yielding the carbamate (IV).The condensation of (IV) with 4-fluorobenzyl chloride (V) by means of K2CO3 in DMF affords N-(benzyloxycarbonyl)-N'-[1-(4-fluorobenzyl)benzimidazol-2-yl)-N,N'-dimethylpropylene-1,3-diamine (VI),which is deprotected with trifluoroacetic acid providing the secondary amine (VII).Finally,this compound is condensed with phenyl N-[3,5-bis(trifluoromethyl)benzyl]carbamate (VIII) by heating at 120 C.
📌 参考资料/链接:
参考文献标题:Benzimidazole deriv.
文献作者:Kamikawaji,Y.; Tanikawa,K.; Yamamoto,A.; Hirotsuka,M.; Iwama,T.; Fujita,Y.(Nissan Chemical Industry,Ltd.)
参考来源:EP 0980359; JP 1999315071; US 6114369; WO 9850368