Libraries from Libraries: A Series of Sulfonamide Linked Heterocycles Derived from the Same Scaffold

Ginamarie Debevec; Wenteng Chen; Yongping Yu; Richard A Houghten; Marc A Giulianotti

doi:10.1016/j.tetlet.2013.06.003

Libraries from Libraries: A Series of Sulfonamide Linked Heterocycles Derived from the Same Scaffold

Tetrahedron Lett. 2013 Aug 7;54(32):10.1016/j.tetlet.2013.06.003. doi: 10.1016/j.tetlet.2013.06.003.

Authors

Ginamarie Debevec¹, Wenteng Chen², Yongping Yu³, Richard A Houghten¹, Marc A Giulianotti¹

Affiliations

¹ Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port St. Lucie FL 34987.
² Torrey Pines Institute for Molecular Studies, 11350 SW Village Parkway, Port St. Lucie FL 34987 ; Institute of Materia Medica, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, P. R. China.
³ Institute of Materia Medica, College of Pharmaceutical Sciences, Zhejiang University, Hangzhou 310058, P. R. China.

Abstract

A libraries from libraries approach is described for the synthesis of five different sulfonamide linked scaffolds. Four of the scaffolds are sulfonamides linked to heterocycles; piperazine, thiourea, cyclic guanidine, and dimethyl cyclic guanidine. The fifth scaffold is a polyamine linked sulfonamide. Three different diversity positions were effectively incorporated into each scaffold providing a number of different compounds with good yields and purity.

Keywords: guanidine; libraries from libraries; piperazine; positional scanning; sulfonamide; urea.

Grants and funding

R01 DA031370/DA/NIDA NIH HHS/United States