Electric Literature of 77112-53-9,Some common heterocyclic compound, 77112-53-9, name is Imidazo[1,2-a]pyrazine-2-carboxylic acid, molecular formula is C7H5N3O2, 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.
Under Ar protection, triethylamine (13.1g, 0.12mol) slowly at 0-5 C was added dropwise a toluene solution of compound 85, and stirred for 30 minutes, slowly added diphenylphosphoryl azide ester (23.61g, 85.79mmol), plus complete slowly warmed to room temperature and stirred for 3 h, then slowly added t-butanol (in 50.0 mL), and the mixture was heated to 80 C, stirred overnight, cooled to room temperature, the reaction mixture under reduced pressure concentrated to dryness and the residue dissolved in ethyl acetate, the organic phase was washed three times with saturated NaCl solution, dried over anhydrous Na2SO4Dried, filtered, and evaporated to dryness and the residue was separated by column chromatography (ethyl acetate: petroleum ether = 1: 4-1: 2) to give compound 86 as a white solid, a total of 5.54g (23.58mmol), a yield of 55.0%.
The synthetic route of 77112-53-9 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; Chinese Academy of Sciences, Shanghai Institute of Medicine; Nanjing Changao Pharmaceutical Technology co., LTD; YANG, YU SHE; CAO, XU FENG; LI, ZHAN; LI, WEI; (78 pag.)CN103965194; (2016); B;,
Pyrazine – Wikipedia,
Pyrazine | C4H4N2 – PubChem