Method for the preparation of crystalline...

C - Chemistry – Metallurgy – 07 – D

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C07D 409/12 (2006.01) C07D 337/08 (2006.01) C07D 409/10 (2006.01) C07D 487/08 (2006.01)

Patent

CA 2460330

Among its several embodiments, the present invention provides an improved process for the preparation of tetrahydrobenzothiepine-1,1-dioxide compounds; the provision of a process for preparing a diastereomeric mixture of tetrahydrobenzothiepine-1,1-dioxide compounds from a single diastereomer of such compounds; the provision of a process for the preparation of 3-bromo-2- substituted propionaldehyde compounds; the provision of a process for the preparation of 3-thio-2-substituted propionaldehyde compounds; and the provision of a process for the preparation of single crystals of ASBT inhibitors having high purity and low levels of solvent impurities.

Parmi les différents modes de mise en oeuvre, l'invention propose un procédé amélioré de préparation de composés tétrahydrobenzothiépine-1,1-dioxide; un procédé de préparation d'un mélange diastéréomère de composés tétrahydrobenzothiépine-1,1-dioxide à partir d'un diastéréomère unique de ces composés; un procédé de préparation de composés 3-bromo-2-propionaldéhyde substitué; un procédé de préparation de composés 3-thio-2-propionaldéhyde substitué; et un procédé de préparation de monocristaux d'inhibiteurs d'ASBT d'une haute pureté et à faibles taux d'impuretés de solvant.

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