新产品编号:81191

Chemical Name: N-[4-[5-(3-Pyridylmethyl)-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-5-ylcarbonyl]phenyl]biphenyl-2-carboxamide
CAS No. 159589-32-9
项目整合开发状态: Preclinical
项目研究机构: Yamanouchi (Originator)
合成路线:Alkylation of benzodiazepinone (I) with 3-(chloromethyl)- pyridine (II) in the presence of NaH gave the 1-substituted benzodiazepinone (III).Reduction of the amide group of (III) with borane in THF afforded benzodiazepine (IV).Subsequent condensation with 4-nitrobenzoyl chloride (V) gave nitrobenzamide (VI),which was reduced to amine (VII) by hydrogenation in the presence of Pd/C.This compound was coupled with acid chloride (IX) (prepared by treatment of 2-phenylbenzoic acid (VIII) with oxalyl chloride) to yield the title compound.
📌 参考资料/链接:
参考文献标题:Nonpeptide arginine vasopressin antagonists for both V1A and V2 receptors: Synthesis and pharmacological properties of 2-phenyl-4'-(2,3,4,5-tetrahydro-1H-1,5-benzodiazepine-1-carbonyl)benzanilide derivatives
文献作者:Matsuhisa,A.; Koshio,H.; Sakamoto,K.; Taniguchi,N.; Yatsu,T.; Tanaka,A.
参考来源:Chem Pharm Bull 1998,46(10),1566