Processing

Please wait...

Settings

Settings

Goto Application

1. WO2010001407 - SYNTHESIS OF 11-(4-[2-(2-HYDROXYETHOXY)ETHYL]- PIPERAZINYL)DIBENZO[B,F][1,4]THIAZEPINE AND ITS FUMARATE SALT

Note: Text based on automatic Optical Character Recognition processes. Please use the PDF version for legal matters

[ EN ]

We Claim :

1. A process for making 1 l-piperazinyldibenzo[b,f][l,4]thiazepine dihydrochloride, the method comprising a. dissolving dibenzo[b,fJ[l,4]thiazepine-ll(10H)one in a non-aromatic solvent and contacting it with phosphorous oxychloride, in the presence of an organic base and phase transfer catalyst, to produce 1 1-chloro- dibenzo[b,fj[l,4]thiazepine as in-situ intermediate. b. adding piperazine to product of step a) in presence of a solvent to produce 1 lpiperazinyldibenzo[b,fj[l,4]thiazepine c. if, necessary the product of step b) can be isolated as dihydrochloride salt by reacting with alcoholic hydrochloride.

2. The process of claim 1 step a) wherein the non-aromatic solvent is acetonitrile or sulfolane.

3. The process of claim 1 step a) wherein the phase transfer catalyst is tetrabutylammonium bromide.

4. The process of claim 1 step a) wherein the base is N,N-dimethyl aniline or triethylamine.

5. The process of claim 1 step b) wherein the solvent is toluene.

6. The process of claim 1 step c) wherein the alcoholic hydrochloride is ethanolic or methanolic.

7. A process for makirig Quetiapine hemifumarate, the process comprising a. alkylating 1 l-piperazinyldibenzo[b,fj[l,4]thiazepine dihydrochloride obtained in claim 1 with 2-(2-chloroethoxy)ethanol in presences of a base, an activator and N-methylpyrrolidine in toluene to get free base of Quetiapine.

b. Contacting the Quetiapine base with fumaric acid in presence of an alcohol.

8. The process of claim 7 step a) Quetiapine base is isolated in-situ. 5

9. The process of claim 7 step a) the base is sodium carbonate; the activator is sodium iodide.

10. The process of claim 7 step b) the alcohol is ethanol, methanol and 10 isopropanol.

15

20

25

30