XR-9051

苯扎米,N-[2-[(3,4-二氢-6,7-二甲氧基-2(1H)-异喹啉基)乙基]苯基]-3-[(Z)-[(5Z)-4-甲基-3,6-二氧基-5-(苯甲基)哌拉嗪酰idene]甲基]-,单盐酸盐Chemical Name: 3-[(3Z,6Z)-6-Benzylidene-1-methyl-2,5-dioxopiperazin-3-ylidenemethyl]-N-[4-[2-(6,7-dimethoxy-1,2,3,4-tetrahydroisoquinolin-2-yl)ethyl]phenyl]benzamide hydrochloride
CAS No. 180422-22-4
项目整合开发状态: Phase I
项目研究机构: Xenova (Originator)
合成路线:Condensation of 1,4-diacetyl-2,5-piperazinedione (I) with the equimolecular amount of benzaldehyde in the presence of triethylamine affords the benzylidene compound (II),which is N-methylated on treatment with iodomethane and sodium hydride to give III.Alkylation of the tetrahydroisoquinoline (V) with 4-(2-bromoethyl)nitrobenzene (IV) provides the tertiary amine (VI).The nitro group of (VI) is reduced by treatment with iron powder and concentrated HCl in refluxing MeOH to give aniline VII,which is condensed with 3-formylbenzoic acid (VIII) in the presence of 2-chloro-1-methylpyridinium iodide to afford the corresponding amide (IX).Finally,condensation between the previously obtained piperazinedione (III) and aldehyde (IX) in the presence of Cs2CO3 leads to the title compound.