Synthetic Route of 773134-11-5, Each compound has different characteristics, and only by selecting the characteristics of the compound suitable for a specific situation can the compound be applied on a large scale. 773134-11-5, name is Methyl 4-bromo-2,6-difluorobenzoate, This compound has unique chemical properties. The synthetic route is as follows.
To a 50 mL round-bottom flask was added (1S,4S,5R)-5-[[4-cyclopropyl-l-(2,6- dichlorophenyl)-1H-pyrazol-5-yl]methoxy]-2-azabicyclo[2.2.1]heptane li (117 mg, 0.31 mmol, 1.00 equiv.), toluene (3 mL), methyl 4-bromo-2,6-difluorobenzoate (85 mg, 0.34 mmol, 1.10 equiv.), Ruphos precatalyst (53 mg, 0.06 mmol, 0.20 equiv.), Ruphos (29 mg, 0.06 mmol, 0.20 equiv.), and Cs2CO3 (303 mg, 0.93 mmol, 3.00 equiv.). The resulting mixture was heated at 110C overnight and concentrated under vacuum. The residue was purified by silica gel column chromatography eluting with ethyl acetate/petroleum ether (1 : 1) to give methyl 4-[(1S,4S,5R)-5- [[4-cyclopropyl-l-(2,6-dichlorophenyl)-1H-pyrazol-5-yl]methoxy]-2-azabicyclo[2.2.1]heptan-2- yl]-2,6-difluorobenzoate 3a (80 mg, 47%) as a light yellow solid.
The chemical industry reduces the impact on the environment during synthesis Methyl 4-bromo-2,6-difluorobenzoate. I believe this compound will play a more active role in future production and life.
Reference:
Patent; ARDELYX, INC.; CHAO, Jianhua; (231 pag.)WO2019/55808; (2019); A1;,
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