Kilogram-scale synthesis of the CXCR4 antagonist GSK812397

S Boggs, VI Elitzin, K Gudmundsson…

Index: Boggs, Sharon; Elitzin, Vassil I.; Gudmundsson, Kristjan; Martin, Michael T.; Sharp, Matthew J. Organic Process Research and Development, 2009 , vol. 13, # 4 p. 781 - 785

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Citation Number: 17

Abstract

CXC chemokine receptor 4 (CXCR4) is a 7-transmembrane protein which functions in part as a host co-receptor for a number of HIV-1 strains.(1) It is believed that targeting CXCR4 would be beneficial in suppressing the replication of several cytopathic late-stage viruses; therefore, CXCR4 antagonists are among the most promising new classes of experimental anti-HIV drugs.(2, 3) GSK812397 is a potent antagonist of CXCR4,(4) and thus a ...