Process and intermediates for preparing ticrynafen

C - Chemistry – Metallurgy – 07 – D

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260/513.4, 260/3

C07D 333/12 (2006.01) C07C 51/00 (2006.01) C07C 65/21 (2006.01) C07D 333/22 (2006.01)

Patent

CA 1081239

ABSTRACT OF THE DISCLOSURE A Reimer-Tiemann reaction of 2,3-dichlorophenol with carbon tetrachloride gives 2,3-dichloro-4-hydroxy- benzoic acid, a novel intermediate, which is then reacted with thiophene in the presence of phosphorus pentoxide or polyphosphoric acid to give 2,3-dichloro-4-(2-thienoyl)- phenol. This compound is then converted to the diuretic, ticrynafen, by known prior art reactions.

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