Proteasome inhibitors

摘要

The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

主权项

1. A process for generating a compound of Formula (v) wherein Ring A is selected from the group consisting of the process comprising:
(1) reacting a compound of Formula (i) with a compound of Formula (ii) to form a compound of Formula (iii) wherein PG is a protecting group; wherein Z1 and Z2, together with the Boron atom to which they are attached, form a boronic ester protecting group; wherein X1− is a counter anion;
(2) deprotecting the compound of Formula (iii) to form a compound of Formula (iiia); wherein X2 is a counter anion;
(3) reacting the compound of Formula (iiia) with a compound of Formula (viii) to form a compound of Formula (iv); and (4) deprotecting the compound of Formula (iv) to form the compound of Formula (v).