Processes for preparing 1,5-benzothiazepine derivatives

Details Processes for preparing 1,5-benzothiazepine derivatives Processes for preparing 1,5-benzothiazepine derivatives

C - Chemistry, Metallurgy

07

D

260/238.6

C07D 281/10 (2006.01)

Patent

CA 2037298

There is disclosed a process for preparing 1,5- benzothiazepine derivatives of the formula: Image wherein R 1 is a lower alkyl group or a salt thereof, which comprises subjecting a propionate derivative of the formula: Image wherein R 2 is a lower alkyl group and R 1 is the same as defined above, to intramolecular cyclization in the presence of a sulfonic acid compound of the formula: R 3SO3H (III) wherein R 3 is a lower alkyl group or a substituted or unsubstituted phenyl group, in a non-halogenated organic solvent and, if desired, converting the product to a salt thereof.

Méthode pour préparer des dérivés de 1,5-benzothiazépine de formule Image , où R1 est un alkyle inf. ou un sel de ce dernier. La méthode consiste à soumettre un propionate de formule Image , où R2 est un alkyle inf. et R1 est tel que défini ci-dessus, à une cyclisation intramoléculaire en présence d'un acide sulfonique de formule R3SO3H (III), où R3 est un alkyle inf. ou un phényle avec ou sans substitution, dans un solvant organique non halogéné et, si souhaitable, à la conversion du produit en son sel.

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