【药物名称】SB-399885
化学结构式(Chemical Structure):
参考文献No.54299
标题:N-(3,5-Dichloro-2-methoxyphenyl)-4-methoxy-3-piperazin-1-yl-benzenesulfonamide
作者:Bromidge, S.M.; Moss, S.F. (GlaxoSmithKline plc)
来源:EP 1313720; WO 0218358
合成路线图解说明:

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)

合成路线图解说明:

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

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