Process for preparing benzothiazepines from...

C - Chemistry – Metallurgy – 07 – D

Patent

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Details

IPC codes

C07D 281/08 (2006.01) C07D 281/10 (2006.01)

Type

Patent

Patent number

CA 2717523

Description

The invention provides a process for preparing a 2,3,4,5--tetrahydro[1,4]benzothiazepine of formula: [I] by reacting a [2--(acylaminoethyl)thio]arene of formula [II] with an aldehyde or a multimer thereof, and with an acid. The invention also provides for first reacting the [2--(acylaminoethyl)thio]arene with the aldehyde or multimer thereof and a base to form an [N-hydroxymethyl-2-[acylaminoethyl)thio]arene of formula [III]; then treating the [N--hydroxymethyl-2-(acylaminoethyl)thio]arene with the acid to form the 2,3,4,5-tetrahy-dro[1,4]benzothiazepine.

L'invention concerne un procédé pour préparer un 2,3,4,5-tétrahydro[1,4]benzothiazépine de la formule suivante : [insérer ici la formule chimique sil vous plaît] en mettant à réagir un [2-(acylaminoéthyl)thio]arène de la formule suivante [insérer ici la formule chimique sil vous plaît] avec un aldéhyde ou un multimère de celui-ci, et avec un acide. L'invention consiste aussi à faire tout d'abord réagir le [2-(acylaminoéthyl) thio]arène avec l'aldéhyde ou le multimère de celui-ci et une base pour former un [N-hydroxyméthyl-2-[acylaminoéthyl)thio]arène de la formule suivante [insérer ici la formule chimique sil vous plaît], puis à traiter le [N-hydroxyméthyl-2-(acylaminoéthyl) thio]arène avec l'acide pour former le 2,3,4,5-tétrahydro[1,4] benzothiazépine.

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