PNU-177864

Chemical Name: N-[4-[2-(Propylamino)ethyl]phenyl]-4-(trifluoromethoxy)benzenesulfonamide
CAS No. 250266-51-4
项目整合开发状态: Preclinical
项目研究机构: Pfizer (Originator)
合成路线:4-Nitrophenethylamine (I) was acylated with propionyl chloride and the resulting amide (II) was reduced to amine (III) with borane-dimethyl sulfide complex in refluxing THF.Amine (III) was then protected as the tert-butyl carbamate (IV) using Boc2O in THF.Subsequent catalytic hydrogenation of the nitro group of (IV) over Pd/C furnished aniline (V),which was coupled with 4-(trifluoromethoxy)benzenesulfonyl chloride (VI) to yield sulfonamide (VII).The Boc protecting group of (VII) was finally removed by treatment with trifluoroacetic acid.