Process for preparing quetiapine and quetiapine fumarate

Details Process for preparing quetiapine and quetiapine fumarate Process for preparing quetiapine and quetiapine fumarate

A - Human Necessities

61

K

A61K 31/554 (2006.01) A61K 9/14 (2006.01) A61K 47/12 (2006.01) A61P 25/18 (2006.01) C07C 57/15 (2006.01) C07D 281/16 (2006.01)

Patent

CA 2605473

The invention comprises a process for preparing quetiapine and/or its salts, including, quetiapine fumarate. The process generally comprises reacting dibenzothiazepinone (dibenzo[bf][l,4]thiazepin-l l(10H)-one) with phosphorous oxychloride in the presence of triethylamine in an aromatic organic solvent such as toluene or, preferably, xylene at reflux temperature to obtain an aromatic hydrocarbon solution of 11-chloro-dibenzo [bf] [1,4] thiazepine. Thereafter, the l l-chloro-dibenzo[bf][1,4] thiazepine is reacted with 2-(2- piperazin-l-ylethoxy)-ethanol to yield, following several processing steps, quetiapine.. Compound I can then be further reacted with fumaric acid at elevated temperature to yield quetiapine fumarate. The resulting quetiapine fumarate obtained is suitable for use in pharmaceutical preparations.

La présente invention concerne un procédé de fabrication de quétiapine et/ou de ses sels, notamment de fumarate de quétiapine. Le procédé consiste à faire réagir dibenzothiazépinone (dibenzo[bf][1,4]thiazépin-11(10H)-one) avec de l'oxychlorure phosphoreux en présence de triéthylamine dans un solvant organique aromatique tel que toluène, de préférence xylène, à une température de reflux de manière à obtenir une solution d'hydrocarbure aromatique de 11-chloro-dibenzo[bf][1,4]thiazépine. La 11-chloro-dibenzo[bf][1,4]thiazépine est ensuite mise en réaction avec 2-(2-pipérazin-1-yléthoxy)-éthanol de manière à former de la quétiapine après diverses étapes de traitement. Le composé (1) peut être mis en réaction ultérieure avec de l'acide fumarique à température élevée de manière à former du fumarate de quétiapine. Le fumarate de quétiapine obtenu peut être employé dans des préparations pharmaceutiques.

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