SB-258741

4-甲基-1-[2-[1-(3-甲基苯基磺酰)吡咯里丁-2(R)-酰基]乙基哌啶Chemical Name: 4-Methyl-1-[2-[1-(3-methylphenylsulfonyl)pyrrolidin-2(R)-yl]ethyl]piperidine
CAS No. 201038-58-6
项目整合开发状态: Preclinical
项目研究机构: GlaxoSmithKline (Originator)
合成路线:Treatment of (R)-2-pyrrolidine methanol (I) with di-tert-butyl dicarbonate and K2CO3 gave carbamate (II),which was converted to mesylate (III) using methanesulfonyl chloride and Et3N.Subsequent reaction of (III) with NaCN in DMF provided nitrile (IV).The catalytic hydrogenation of this nitrile in the presence of 4-methylpiperidine (V) furnished the (piperidinylethyl)pyrrolidine (VI).After Boc deprotection of (VI) with trifluoroacetic acid in refluxing CH2Cl2,the resulting pyrrolidine (VII) was finally condensed with m-toluenesulfonyl chloride (VIII) to give the target sulfonamide.