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

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

Volume: 13 Issue: 5

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

Affiliation:

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

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.

Cite this article as:

Yerrabelly Rao Jayaprakash, Rebelli Pradeep, Yalamanchili Kumari Bharathi and Ghojala Reddy Venkat, A New and Convenient Synthesis of the Boceprevir P1 Fragment, β-amino-α-Hydroxy Amide, Letters in Organic Chemistry 2016; 13 (5) . https://dx.doi.org/10.2174/1570178613666160628090059