3-hydroxymethyl-benzo[b]thiophene derivatives and process...

Details 3-hydroxymethyl-benzo[b]thiophene derivatives and process... 3-hydroxymethyl-benzo[b]thiophene derivatives and process...

C - Chemistry, Metallurgy

07

D

C07D 333/56 (2006.01) C07D 333/64 (2006.01)

Patent

CA 2414298

A process for preparing 3-hydroxymethylbenzo[b]- thiophene derivatives according to the following reaction scheme without the formation of isomers, which comprises selectively cyclizing an X-containing sulfoxide and then selectively replacing the X by hydrogen: wherein R1 to R3 are each independently hydrogen, C1-4 alkyl, trihalomethyl, C1-4 alkoxy, C1-4 alkylthio, or trihalomethoxy; R4 is acyl; and X is halogeno, hydroxyl, amino, mercapto, C1-9 alkylthio, C1-9 acyloxy, C1-9 acylamino, or trihalomethoxy.

L'invention concerne un procédé de préparation de dérivés de 3-hydroxyméthylbenzo[b]thiopène selon le système de réaction suivant sans formation d'isomères consistant à cycliser de manière sélective un sulfoxyde contenant X puis à remplacer de manière sélective X par de l'hydrogène. R¿1?, R¿2 ?et R¿3? sont chacun indépendamment hydrogène, C¿1-4 ?alkyle, trihalométhyle, C¿1-4 ?alkoxy, C¿1-4 ?alkylthio, ou trihalométhoxy ; R¿4? est acyle ; et X est halogéno, hydroxy, amino, mercapto, C¿1-9? alkylthio, C¿1-9 ?acyloxy, C¿1-9 ?acylamino, ou trihalométoxy.

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