Practical synthesis of 6-Amino-1-hydroxy-2,1-benzoxaborolane: A key intermediate of DNDI-6148

By Khairnar PV, Saathoff JM, Cook DW, Hochstetler SR, Pandya U, Robinson SJ, Satam V, Donsbach KO, Gupton BF, Jin L-M, Shanahan CS. Organic Process Research & Development 2024. doi: 10.1021/acs.oprd.4c00031

Summary: DNDI-6148 is a promising drug candidate under evaluation for the treatment of visceral leishmaniasis, however, the current process for producing the key intermediate, 6-amino-1-hydroxy-2,1-benzoxaborolane, is expensive and difficult to scale up. The authors of this manuscript describe two practical approaches to synthesizing this intermediate from inexpensive and readily available raw materials. With studies showing that, in addition to visceral leishmaniasis, DNDI-6148 could potentially be developed for treatment of cutaneous leishmaniasis and Chagas disease, this work could have a significant impact on enabling access of DNDI-6148 to those in dire need.

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