Nucleoside Reverse Transcriptase Inhibitors (NRTI's) were first synthesized in the 1960's and have been developed for the treatment of the HIV virus for the last 30 years. BMS-986001 is an  investigational nucleoside analog  being developed as a potential new treatment in this area, and the development of a safe, efficient and economical synthesis of this compound was critical to its continued development. In this communication, we discuss the design and execution of a new stereocontrolled synthesis of BMS-986001.  The synthesis features the construction of stereogenic centers by way of reagent and substrate control, resulting in a short and efficient route from commercially available achiral starting materials.

Discovery of an innovative stereoselective synthesis of BMS-986001: A nucleoside reverse transcriptase inhibitor (NRTI) for the treatment of HIV infection

248th National Meeting (2014)

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