新产品编号:2321303

Chemical Name: N1,N4-Bis[3-oxo-3-(9H-purin-6-ylsulfanylmethoxy)propyl]-N2-[2-(polyethyleneglycol)ethoxycarbonyl]-L-asparaginamide
项目整合开发状态: Preclinical
项目研究机构: Enzon (Originator)
合成路线:Treatment of N-Boc-beta-alanine (I) with bromochloromethane gives the chloromethyl ester (II),which is further converted to the iodomethyl analogue (III) under the Finkelstein halide exchange reaction conditions.Condensation of iodomethyl ester (III) with 6-mercaptopurine (IV) provides adduct (V).The N-Boc group of (V) is then removed employing trifluoroacetic acid to furnish the amine compound (VI).Finally,EDC-mediated coupling of amine (VI) with the polyethyleneglycol-bound aspartic acid (VII) affords the title mercaptopurine prodrug.