SB-399885

N-(3,5-二氯-2-甲氧基苯基)-4-甲氧基-3-(1-哌嗪基)苯磺酰胺 盐酸盐N-(3,5-二氯-2-甲氧基苯基)-4-甲氧基-3-(1-哌嗪基)苯磺酰胺盐酸盐Chemical Name: N-(3,5-Dichloro-2-methoxyphenyl)-4-methoxy-3-(1-piperazinyl)benzenesulfonamide
CAS No. 402713-80-8, 402713-82-0 (4-methylbenzenesulfonate), 402713-81-9 (hydrochloride)
项目整合开发状态: Preclinical
项目研究机构: GlaxoSmithKline (Originator)
合成路线:N-(2-Methoxyphenyl)piperazine (I) is protected as the trichloroacetamide (II) using trichloroacetyl chloride and diisopropylethylamine.Then,chlorosulfonation of (II) in cold CH2Cl2 furnishes sulfonyl chloride (III)

合成路线:Alkylation of 2,4-dichloro-6-nitrophenol (IV) with iodomethane in the presence of K2CO3 provides the methyl ether (V).Subsequent nitro group reduction in (V) employing iron powder and NH4Cl leads to aniline (VI).This is then acylated by sulfonyl chloride (III) to form sulfonamide (VII).The N-trichloroacetyl group of (VII) is finally removed by alkaline hydrolysis to provide the title compound