-药物合成数据库

【药物名称】

化学结构式(Chemical Structure):

参考文献No.	45799
标题:	Thiazepine inhibitors of HIV-1 integrase
作者:	Garofalo, A.; Pommier, Y.; Neamati, N.; Nacci, V. (US Department of Health & Human Services)
来源:	WO 0068235

合成路线图解说明: Treatment of 2,2'-dithiobis(benzoic acid) (I) with thionyl chloride produced the corresponding acid chloride (II), which was further condensed with thiazolidine-2-carboxylic acid (III) in the presence of Na2CO3 to furnish diamide (IV). Reductive cleavage of the disulfide group of (IV) by means of NaBH4 in refluxing EtOH yielded thiol (V). Finally, intramolecular cyclization of (V) to give the title tricyclic compound was achieved by treatment with carbonyl diimidazole in boiling THF.

参考文献No.	547222
标题:	Thiazolothiazepine inhibitors of HIV-1 integrase
作者:	Neamati, N.; Turpin, J.A.; Winslow, H.E.; Christensen, J.L.; Williamson, K.; Orr, A.; Rice, W.G.; Pommier, Y.; Garofalo, A.; Brizzi, A.; Campiani, G.; Fiorini, I.; Nacci, V.
来源:	J Med Chem 1999,42(17),3334

合成路线图解说明: Treatment of 2,2'-dithiobis(benzoic acid) (I) with thionyl chloride produced the corresponding acid chloride (II), which was further condensed with thiazolidine-2-carboxylic acid (III) in the presence of Na2CO3 to furnish diamide (IV). Reductive cleavage of the disulfide group of (IV) by means of NaBH4 in refluxing EtOH yielded thiol (V). Finally, intramolecular cyclization of (V) to give the title tricyclic compound was achieved by treatment with carbonyl diimidazole in boiling THF.