Share a compound : 5-(Difluoromethyl)pyrazine-2-carboxylic acid

The synthetic route of 1174321-06-2 has been constantly updated, and we look forward to future research findings.

Synthetic Route of 1174321-06-2, A common heterocyclic compound, 1174321-06-2, name is 5-(Difluoromethyl)pyrazine-2-carboxylic acid, molecular formula is C6H4F2N2O2, 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 an ice-water cooled mixture of tert-butyl[(4’R)-6′-amino-2′,2′-dimethyldispiro[cyclopropane-1,3′-chromene-4′,4″-[1,3]oxazol]-2″-yl]carbamate (430 mg, 1.15 mmol), 5-(difluoromethyl)pyrazine-2-carboxylic acid (221 mg, 1.27mmol) and lH-benzotriazol-1-ol (170 mg, 1.26 mmol) in chloroform (8.6 ml) was addedN-[3-(dimethylamino)propyl]-N’-ethylcarbodiimide hydrochloride (244 mg, 1.28 mmol). Themixture was stirred at room temperature overnight and directly purified by silica gel columnchromatography (precolumn: basic silica gel, main column: neutral silica gel, hexane/ethylacetate= 2:1- 1:1- 0:100) to afford tert-butyl[ ( 4’R)-6′-( { [5-( difluoromethyl)pyrazin-2-yl]carbonyl }amino )-2′ ,2′-dimethyldispiro[ cyclopropane-1,3′-chromene-4′,4″-[1,3]oxazol]-2″-yl]carbamate (373 mg).

The synthetic route of 1174321-06-2 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; ASTELLAS PHARMA INC.; COMENTIS, INC.; MUNAKATA, Ryosuke; INOUE, Makoto; TOMINAGA, Hiroaki; YAMASAKI, Shingo; SHIINA, Yasuhiro; SAMIZU, Kiyohiro; HAMAGUCHI, Hisao; HONG, Lin; WO2013/181202; (2013); A2;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem