Crystalline compound of 7-[(3R)-3-amino-1-oxo-4-(2, 4, 5-trifluorophenyl)butyl]-5, 6, 7, 8-tetrahydro-3-(tri fluoromethyl)-1, 2, 4 -triazolo[4,3-A]pyrazin

摘要

A crystalline compound of 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazine (INN: Sitagliptin) of formula 1;
with fumaric acid or a hydrate thereof, where the molar ratio of the compound of formula 1 to fumaric acid is 1:0.6 to 1:1.3 is described.

主权项

1. A crystalline compound of 7-[(3R)-3-amino-1-oxo-4-(2,4,5-trifluorophenyl)butyl]-5,6,7,8-tetrahydro-3-(trifluoromethyl)-1,2,4-triazolo[4,3-a]pyrazine (INN: Sitagliptin) of formula 1with fumaric acid thereof, where the molar ratio of the compound of formula 1 to fumaric acid is 1:0.95 to 1:1.05, which has, by means of x-ray powder diffractometry (XRPD) d values (A) at 12.9 (w), 10.3 (w), 5.15 (m) and 4.30 (vs), which is subsequently referred to as form A.