Abstract: The invention relates to a process for simultaneously N(2)-acylating piperazic acid or an ester thereof and forming a bicyclic ring structure. The invention also relates to the use of that process step in a method of synthesizing a bicyclic compound useful as an intermediate for the production of an inhibitor of a caspase, particularly an inhibitor of interleukin-1&bgr; converting enzyme (“ICE”).
Type:
Grant
Filed:
August 19, 1998
Date of Patent:
March 13, 2001
Assignee:
Vertex Pharmaceuticals Inc.
Inventors:
Andrea L. C. Robidoux, Jeffrey Douglas Wilson, Petra Dietrich, Neil Storer, Stefania Leonardi
Abstract: The invention relates to a process for synthesizing piperazic acid and similar, ring-containing acids. The invention also relates to a process for simultaneously N(2)-acylating piperazic acid or an ester thereof and forming a bicyclic ring structure. The invention also relates to the use of either or both processes in a method of synthesizing a bicyclic compound useful as an intermediate for the production of an inhibitor of a caspase, particularly an inhibitor of interleukin-1&bgr; converting enzyme (“ICE”).