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Synthesis and Process Optimization of Boceprevir: A Protease Inhibitor Drug

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journal contribution
posted on 2015-11-20, 00:00 authored by Dinesh S. Bhalerao, Anil Kumar Reddy Arkala, Y. V. Madhavi, M. Nagaraju, Srinivas Reddy Gade, U. K. Syam Kumar, Rakeshwar Bandichhor, Vilas H. Dahanukar
Efforts toward the synthesis and process optimization of boceprevir 1 are described. Boceprevir synthesis was optimized by telescoping the first three steps and last two steps of the five-step process. Optimization of oxidation, which is one of the critical steps in the total synthesis, is discussed. A control strategy for the three impurities is described. A novel process for the synthesis of fragment A (2) has been developed, which is the key starting material for the synthesis of boceprevir.

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