Development of a scalable process for the synthesis of DNDI-VL-2098: A potential preclinical drug candidate for the treatment of VL

by Satam VS, Rao Pedada S, Kamaraj P, Antao N, Singh A, Hindupur RM, Pati HN, Thompson AM, Launay D, Martin DOrg. Proc. Res. Dev. 2017, doi:10.1021/acs.oprd.6b00331.

Summary: This report describes the elaboration of a process suitable for the kilogram scale synthesis of DNDI-VL-2098, a preclinical candidate for the treatment of visceral leishmaniasis. The four step synthesis involves the Sharpless asymmetric epoxidation of one of the intermediates, and was simplified by employing in situ synthesis of some intermediates, thereby reducing safety hazards and eliminating the need for column chromatography. The improved reactions when carried out at kilogram scale produced DNDI-VL-2098 in good yield, high optical purity and high quality.

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