Introduction of a new synthetic route about C4H4N4

The synthetic route of 81606-79-3 has been constantly updated, and we look forward to future research findings.

Related Products of 81606-79-3, These common heterocyclic compound, 81606-79-3, name is 2-(1,2,4-Triazol-1-yl)acetonitrile, 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.

To a 25 ml microwave vial, N-((2S,3R)-l -(((S)-l -((2-fluoro-4-methylbenzyl)amino)-3- (3-formylphenoxy)-l-oxopropan-2-yl)amino)-3-hydroxy- l-oxobutan-2-yl)-5-methylisoxazole-3- carboxamide (190 mg, 0.46 mmol) and 2-(l H-l ,2,4-triazol- l -yl)acetonitrile (247 mg, 2.28 mmol) were suspended in toluene (2 ml). TEA (0.15 ml, 1.05 mmol) was added and stirred at 125 C for 1 .5 h in microwave. The reaction mixture was diluted with cold water and extracted with ethyl acetate. The combined organic layer was dried over sodium sulfate, filtered and concentrated to get the crude product which was purified by prep HPLC purification using 0.1 % Formic Acid in water as modifier in acetonitrile to yield 16 mg of N-((2S,3R)-l -(((S)-3-(3-(2- cyano-2-(l H- l ,2,4-triazol-l -yl)vinyl)phenoxy)-l -((2-fluoro-4-methyl benzyl)amino)-l – oxopropan-2-yl)am i no)-3 -hydroxy- 1 -oxobutan-2-yl)-5 -methyl i soxazole-3 -carboxam ide. LC-M S (ES, m/z): 631 [M+H].

The synthetic route of 81606-79-3 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; BRAMELD Kenneth; OWENS Timothy; WO2015/195950; A1; (2015);,
1,2,3-Triazole – Wikipedia,
Triazoles – an overview | ScienceDirect Topics