Process for producing muscarine receptor antagonist and...

C - Chemistry – Metallurgy – 07 – D

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C07D 233/61 (2006.01) A61K 31/4164 (2006.01) A61P 1/06 (2006.01) A61P 1/12 (2006.01) A61P 1/16 (2006.01) A61P 11/00 (2006.01) A61P 13/02 (2006.01) A61P 13/06 (2006.01) A61P 43/00 (2006.01)

Patent

CA 2589146

The industrial production of 4-(2-methyl-1-imidazolyl)-2,2-- diphenylbutanamide, a urinary incontinence remedy, necessitates elimination of problems concerning the use of a synthetic adsorbent, e.g., HP-20, the efficiency of operation with the same, purification efficiency, etc. An acid salt, e.g., hydrochloride or phosphate, of 4-(2-methyl-1-imidazolyl)-2,2- diphenylbutanamide or a hydrate of any of these salts is used as an intermediate. This intermediate is neutralized and then purified. Thus, high-purity 4-(2-methyl-1-imidazolyl)-2,2-diphenylbutanamide is easily obtained in satisfactory yield. The industrial-scale production process has been thus established.

L~invention concerne la production industrielle du 4-(2-méthyl-1-imidazolyl)-2,2-diphénylbutanamide, qui constitue un remède à l~incontinence urinaire. Cette production nécessite d~éliminer les problèmes relatifs à l~utilisation d~un adsorbant synthétique, par exemple HP-20, à l~efficacité de fonctionnement avec ce même adsorbant, à l~efficacité de purification, etc. Un sel acide, par exemple un chlorhydrate ou phosphate, du 4-(2-méthyl-1-imidazolyl)-2,2-diphénylbutanamide ou un hydrate de n~importe lequel de ces sels est utilisé en tant qu~intermédiaire. Celui-ci est neutralisé puis purifié. On obtient ainsi, facilement et avec un rendement satisfaisant, un 4-(2-méthyl-1-imidazolyl)-2,2-diphénylbutanamide d~une pureté élevée. Ainsi a été établi le procédé de production à échelle industrielle.

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