Pyridine → 2,2-Dimethyl-propionic acid 7-(2-chloro-3,6-difluoro-phenyl)-6-oxo-5,6-dihydro-pyrido[2,3-b]pyrazin-8-yl ester

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Reaction Steps

A mixture of 7-(2-chloro-3,6-difluoro-phenyl)-8-hydroxy-5H-pyrido[2,3-b]pyrazin-6-one (0.20 g) (Example 1.2), trimethylacetyl chloride (0.08 ml), and pyridine (0.05 ml) in dichloromethane (5 ml) was stirred at ambient temperature for two hours. The reaction mixture was diluted with ethyl acetate and water. The phases were separated. The organic phase was dried over magnesium sulfate and concentrated to produce a yellow semi-crystalline oil. This was triturated in iso-hexane to produce 2,2-dimethyl-propionic acid 7-(2-chloro-3,6-difluoro-phenyl)-6-oxo-5,6-dihydro-pyrido[2,3-b]pyrazin-8-yl ester as a pale brown powder (0.113 g). 1H-NMR (400 MHz, CDCl3): 1.21 (s, 9H), 7.08-7.13 (m, 1H), 7.21-7.27 (m, 1H), 8.55-8.57 (m, 2H), 9.51 (s, 1H) ppm.

Provenance & Evidence