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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:
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. KaczmarekSee On-line Journal of V Multidyscyplinarna Konferencja Nauki o Leku Submitted: 2006-01-25 18:37 Revised: 2009-06-07 00:44 |