NEW SYNTHESIS OF 11-(1-PIPERAZINYL)- DIBENZO[b,f][1,4]THIAZEPINE, A CRUCIAL INTERMEDIATE IN QUETIAPINE PRODUCTION.

Łukasz S. Kaczmarek ,  Katarzyna Badowska-Rosłonek ,  Elżbieta U. Stolarczyk ,  Teresa Paszkowska-Reymer 

Pharmaceutical Research Institute (IF), Rydygiera 8, Warszawa 01-793, Poland

Abstract

Quetiapine is a novel antipsychotic drug, showing higher activity and fewer side effects than the classical antypsychotic agents. 11-(1-Piperazinyl)dibenzo[b,f][1,4]thiazepine is the crucial intermediate in the synthesis of quetiapine:


q_1.JPG

Our invention1 relates to the process of the preparation of this intermediate. In comparison with the classical industrial method2 ours offers several advantages, i.e.:

- reduction of operations number and time; - higher total yield (75% vs. 60%); - lower consumption of solvents; - reduction of waste material quantity;

All these advantages result in considerable reduction of manufacturing costs.

1 Ł. Kaczmarek, K. Badowska-Rosłonek, E. Stolarczyk, W. Szelejewski, " Process for preparation of 11-(1-piperazinyl)dibenzo[b,f][1,4]thiazepine, an intermediate in the synthesis of the antipsychotic drug Quetiapine.", PCT/EP2004/051520 (2004).

2 EP 0240228

 

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Presentation: Poster at V Multidyscyplinarna Konferencja Nauki o Leku, by Łukasz S. Kaczmarek
See On-line Journal of V Multidyscyplinarna Konferencja Nauki o Leku

Submitted: 2006-01-25 18:37
Revised:   2009-06-07 00:44