NU-1025

2-甲基-8-羟基-4-喹唑啉酮Chemical Name: 8-Hydroxy-2-methylquinazolin-4(3H)-one
CAS No. 90417-38-2
项目整合开发状态: Preclinical
项目研究机构: Agouron (Originator), Cancer Research UK (Originator), University of Newcastle upon Tyne (Originator)
合成路线:Thus,benzoxazole-4-carboxylate (I) was rearranged in ammonia at 55 C under pressure to give the target 8-hydroxy-2-methylquinazolin-4-one,although in modest yields.

合成路线:In an alternative procedure,3-methoxy-2-nitrobenzoic acid (II) was treated with SOCl2 in the presence of DMF in THF,and the resulting acid chloride (III) was converted to amide (IV) with aqueous ammonia.Catalytic hydrogenation of (IV) over Pd/C produced aniline (V),which was then acetylated with AcCl and pyridine.The crude acetylamino compound (VI) was cyclized by treatment with aqueous NaOH to yield the quinazolinone (VII).Finally,demethylation of the methoxy group of (VII) with BBr3 provided the required 8-hydroxyquinazolinone.