Process for preparing benzothiophenecarboxamide derivatives

Details Process for preparing benzothiophenecarboxamide derivatives Process for preparing benzothiophenecarboxamide derivatives

C - Chemistry, Metallurgy

07

D

C07D 333/68 (2006.01) C07C 213/00 (2006.01) C07C 213/02 (2006.01) C07C 215/42 (2006.01)

Patent

CA 2326418

A process for producing compounds having PGD2 antagonism represented by formula (I), pharmaceutically acceptable salts thereof or hydrates of the same characterized by reacting an amino alcohol of formula (II) or its salt with a compound of formula (III) or its reactive derivative, oxidizing the obtained product in the presence of 2,2,6,6,-tetramethylpiperidine-1-oxyls, and then reacting with an ylide under Wittig reaction conditions optionally followed by deblocking.

L'invention concerne un procédé de production de composés présentant un antagonisme de PGD¿2? représentés par la formule (I), de leurs sels pharmaceutiquement acceptables ou de leurs hydrates. Ce procédé est caractérisé en ce qu'on fait réagir un amino-alcool de formule (II) ou son sel avec un composé de formule (III) ou son dérivé réactif, on oxyde le produit obtenu en présence de 2,2,6,6,-tétraméthylpipéridine-1-oxyles, puis on fait réagir avec un ylure dans des conditions de réaction de Wittig, éventuellement suivie d'un déblocage.

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