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.
Letters in Organic Chemistry
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.
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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
DOI https://dx.doi.org/10.2174/1570178613666160628090059 |
Print ISSN 1570-1786 |
Publisher Name Bentham Science Publisher |
Online ISSN 1875-6255 |
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