Patent ID: 8962836
Filing Date: 2015-02-24
Classification: C07D

Abstract:
1. A method for the synthesis of a bis N-protected 3,6-aminoalkyl-2,5-diketopiperazine of Formula I, wherein PG is selected from CBz, Boc, trifluoroacetyl, and acetyl and wherein n is from 1 to 8; the method comprising: adding a cyclic α-N protected active amino ester according Formula II wherein PG is selected from CBz, Boc, trifluoroacetyl, and acetyl, wherein X is selected from C, S, and P, and wherein n is from 1 to 8; to a mixture of an amine catalyst in an organic solvent, the amine catalyst selected from the group comprising: aziridine and benzamidoxime.