An Efficient Synthesis of an AKT Inhibitor-IV Analog Labeled with Biotin

An AKTI-IV analog with a biotinylated linker extended from the position of the ethyl group in AKTI-IV have been designed and synthesized. Compared to previous alkylation strategy with the iodo biotin linker, the present method alkylated the linker without biotin moiety. The final biotinylation with biotin-OSU afforded the target molecule in much higher overall yield.