SV-030

Chemical Name: 6-[2-Chloro-4-(trifluoromethyl)phenyl]-9-(dicyclopropylmethyl)-8-ethyl-9H-purine
CAS No. 219733-55-8
项目整合开发状态: Preclinical
项目研究机构: Bristol-Myers Squibb (Originator)
合成路线:Condensation of 5-amino-4,6-dichloropyrimidine (I) with benzylamine afforded diamine (III).Subsequent reaction of (III) with triethyl orthopropionate in the presence of HCl produced imidate (IV),which was cyclized to purine (V) upon heating in diphenyl ether in the presence of p-toluenesulfonic acid.Palladium catalyzed coupling of (IV) with the organozinc derivative generated from Grignard reagent (V) and ZnCl2 produced the corresponding 6-aryl purine (VI).The N-benzyl group of (VI) was then deprotected by hydrogenation in the presence of palladium catalyst and trifluoroacetic acid to furnish (VII).Finally,condensation with dicyclopropylcarbinol (VIII) under Mitsunobu conditions yielded the title compound.