Synthetic Route of 767340-03-4, A common heterocyclic compound, 767340-03-4, name is (2Z)-4-Oxo-4-[3-(trifluoromethyl)-5,6-dihydro[1,2,4]triazolo[4,3-a]pyrazine-7(8H)-yl]-1-(2,4,5-trifluorophenyl)but-2-en-2-amine, molecular formula is C16H13F6N5O, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
(Z)-3-amino-1-(3-(trifluoromethyl)-5,6-dihydro-[1,2,4]triazolo[4,3-a]-pyrazyn-7(8H)-yl)-4-(2,4,5-trifluorophenyl)but-2-en-1-one (10 gr, 1 equivalent) and methanol (50 ml) were added to a 250 ml hydrogenation bottle at 25 C. and the bottle was subjected to vacuum and nitrogen backflush three times. The catalyst solution was added to the hydrogenation bottle and the bottle was again subjected to vacuum and nitrogen backflush three times and then to vacuum and backflush with hydrogen gas three times. The resulting reaction mixture was maintained under hydrogen at a pressure of 5 bar and heated to 55 C. The heated mixture was stirred at 5 bar pressure, at 55 C. for 3 days to obtain Sitagliptin base in methanol solution (optical purity by HPLC 97%, purity by HPLC 63.7%).
The synthetic route of 767340-03-4 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; Teva Pharmaceutical Industries Ltd.; US2010/249140; (2010); A1;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem