Process for preparing quetiapine and quetiapine fumarate

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

2006-04-21

2011-11-01

Coleman, Brenda (Department: 1624)

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Heterocyclic carbon compounds containing a hetero ring...

C540S551000

Reexamination Certificate

active

08048876

ABSTRACT:
The invention comprises a process for preparing quetiapine and/or its salts, including, quetiapine fumarate. The process generally comprises reacting dibenzothiazepinone (dibenzo[bf][1,4]thiazepin-11(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 11-chloro-dibenzo[bf][1,4]thiazepine is reacted with 2-(2-piperazin-1-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.

REFERENCES:
patent: 5286722 (1994-02-01), Cairns et al.
patent: 2005/0003001 (2005-01-01), Yamaguchi et al.
patent: 2006/0063927 (2006-03-01), Etlin et al.
patent: 0 240 228 (1987-10-01), None
patent: 01/21179 (2001-03-01), None
patent: 02/094236 (2002-11-01), None
patent: WO 03/080065 (2003-10-01), None
patent: WO 2004078735 (2004-09-01), None
patent: WO 2006/001619 (2006-01-01), None
International Search Report dated Nov. 21, 2006 for International Patent Application No. PCT/IB2006/002286.
Warawa et al. “Behavioural Approach to Nondynskinetic Dopamine Antagonists: Identification ofSeroquel”, J. Med. Chem., vol. 44, 2001, pp. 372-389.
Schmutz et al. “29. Uber in 11-stellung amino-substitute Dibenzo[b,f]—1,4-thiazepine und—ozazepine”, Helvetica Chimica Acta, vol. 50, 1967, pp. 245-254.
Kuehne et al. “Reduction of Amides and Lactams by Amines by Reactions with Phosphorour Oxychloride and Sodium Borohydride”, J. Org. Chem., vol. 42, No. 12, 1977, pp. 2082-2087.

Affiliated with

Also associated with

Rating

Process for preparing quetiapine and quetiapine fumarate does not yet have a rating. At this time, there are no reviews or comments for this patent.

If you have personal experience with Process for preparing quetiapine and quetiapine fumarate, we encourage you to share that experience with our LandOfFree.com community. Your opinion is very important and Process for preparing quetiapine and quetiapine fumarate will most certainly appreciate the feedback.

Rate now

Comments { 0 }

Profile ID: LFUS-PAI-O-4287691