Dimethylformamide dimethyl acetal → 2-(5-(3-Chloro-2-fluorobenzyl)-2-fluoro-4-methoxybenzoyl)-3-dimethylaminoacrylic acid ethyl ester

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Reaction Steps

To a solution of 3-(5-(3-chloro-2-fluorobenzyl)-2-fluoro-4-methoxyphenyl)-3-oxopropionic acid ethyl ester prepared in Step VI-2 in toluene was added dropwise at 75-85° C., N,N-dimethylformamide dimethyl acetal (5.08 g) with stirring, and the mixture was stirred for 3 hr. After cooling, a solution of 2-(5-(3-chloro-2-fluorobenzyl)-2-fluoro-4-methoxybenzoyl)-3-dimethylaminoacrylic acid ethyl ester in toluene was obtained. This was identified as the title compound by HPLC.

Provenance & Evidence