Tetrahedron

Synthesis of isotopically labelled SGLT inhibitors and their metabolites

V Derdau, T Fey, J Atzrodt

Index: Derdau, Volker; Fey, Thorsten; Atzrodt, Jens Tetrahedron, 2010 , vol. 66, # 7 p. 1472 - 1482

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Citation Number: 11

Abstract

Isotopically labelled analogues of two structurally very similar SGLT inhibitors AVE2268 (1a) and AVE8887 (1b) have been synthesized by various routes. The radioactive labelled [14C]- AVE2268 was prepared in five steps including a Friedel–Crafts acylation as the key step for the 14C-label introduction. For [14C]-AVE8887 the same synthetic approach was not successful and therefore an alternative thiophene metallation/Weinreb amide sequence ...