Letters in Organic Chemistry

Author(s): Jayaprakash Rao Yerrabelly, Pradeep Rebelli, Bharathi Kumari Yalamanchili and Venkat Reddy Ghojala

DOI: 10.2174/1570178613666160628090059

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A New and Convenient Synthesis of the Boceprevir P1 Fragment, β-amino-α-Hydroxy Amide

Page: [352 - 358] Pages: 7

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Abstract

A new and convenient synthesis of the P1 fragment of HCV inhibitor, boceprevir is described. This approach efficiently provides P1 fragment of boceprevir using simple and easy handling reagents suitable for scale up. This synthetic route involves the conversion of ester intermediate into novel intermediate, α-chloro ketone via chloroacetate Claisen condensation, followed by further simple conversions to β-amino-α-hydroxy amide, P1 fragment of boceprevir in high yield.

Keywords: Boceprevir, Chloroacetate Claisen condensation, Convenient synthesis of boceprevir P1 fragment, P1 fragment, α-hydroxy amide.