新产品编号:516241

合成路线:Treatment of N-Boc-prolinol (I) with p-toluenesulfonyl chloride and pyridine afforded tosylate (II),which was condensed with the sodium salt of phenol (III) to produce ether (IV).Acid cleavage of the Boc protecting group of (IV) then gave pyrrolidine (V).Sulfonyl chloride (VII) was prepared by chlorination of the sodium salt of 5-isatinsulfonic acid (VI) with POCl3 in tetramethylenesulfone.Acylation of pyrrolidine (V) with acid chloride (VII) gave sulfonamide (VIII).Finally,the isatin nitrogen atom was methylated employing iodomethane in the presence of K2CO3.

参考文献标题:Caspases and apoptosis
文献作者:Lee,D.; Long,S.A.; Elliott,J.D.; Gleason,J.G.(SmithKline Beecham Corp.)
参考来源:WO 0122966


合成路线:Treatment of N-Boc-prolinol (I) with p-toluenesulfonyl chloride and pyridine afforded tosylate (II),which was condensed with the sodium salt of phenol (III) to produce ether (IV).Acid cleavage of the Boc protecting group of (IV) then gave pyrrolidine (V).Sulfonyl chloride (VII) was prepared by chlorination of the sodium salt of 5-isatinsulfonic acid (VI) with POCl3 in tetramethylenesulfone.Acylation of pyrrolidine (V) with acid chloride (VII) gave sulfonamide (VIII).Finally,the isatin nitrogen atom was methylated employing iodomethane in the presence of K2CO3.
参考文献标题:Potent and selective nonpeptide inhibitors of caspases 3 and 7
文献作者:Lee,D.; Long,S.A.; Murray,J.H.; Adams,J.L.; Nuttall,M.E.; Nadeau,D.P.; Kikly,K.; Winkler,J.D.; Sung,C.M.; Ryan,M.D.; Levy,M.A.; Keller,P.M.; DeWolf,W.E.Jr.
参考来源:J Med Chem 2001,44(12),2015