Pankaj V Khairnar, John M Saathoff, Daniel W Cook, Samuel R Hochstetler, Urvish Pandya, Stephen J Robinson, Vijay Satam, Kai O Donsbach, B Frank Gupton, Li-Mei Jin, Charles S Shanahan
Visceral leishmaniasis (VL), a parasitic, poverty-linked, neglected disease, is endemic across multiple regions of the world and fatal if untreated. There is an urgent need for a better and more affordable treatment for VL. DNDI-6148 is a promising drug candidate being evaluated for the treatment of VL; however, the current process for producing the key intermediate of DNDI-6148, 6-amino-1-hydroxy-2,1-benzoxaborolane, is expensive and difficult to scale up. Herein, we describe two practical approaches to synthesizing 6-amino-1-hydroxy-2,1-benzoxaborolane from inexpensive and readily available raw materials...
April 19, 2024: Organic Process Research & Development