Patent
A PROCESS FOR THE PREPARATION OF 2-[2-(4-DIBENZO[b,f] [L,4] THIAZEPIN-11-yl-1- PIPERAZINYL)ETHOXY] ETHANOL FUMARATE
Venkatasubramanian Radhakrishnan Tarur,Dhananjay Govind Sathe,Avinash Venkataraman Naidu,Umesh Parashram Aher,Sachin Shivaji Patil +4 more
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TLDR
A process for the preparation of 2-(4-Dibenzo[b,f] [l,4] thiazepin-11-yl-1- ρiperazinyl)ethoxy] ethanol fumarate commonly known as Quetiapine hemifumarate is described in this article.Abstract:
A process for the preparation of 2-[2-(4-Dibenzo[b,f] [l,4] thiazepin-11-yl-1- ρiperazinyl)ethoxy] ethanol fumarate commonly known as Quetiapine hemifumarate. Dibenzo[b,f] [l,4] thiazepin-11-[10H]one is halogenated with a halogenating agent in the ratio of 1 : 0.5 to 3 w/v in an organic solvent in the presence of an organic base at reflux temperature followed by condensation of the reaction with piperazine without isolating the imino chloride. The piperazinyl-dibenzo[b,f] [l,4] thiazepine is converted to Quetiapine hemifumarate which is purified by crystallization with alcohol at reflux temperature and precipitated it by cooling the reaction mixture and recovered by filtration.read more
Citations
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Journal ArticleDOI
Generation of Aryl Radicals from Aryl Halides: Rongalite-Promoted Transition-Metal-Free Arylation
TL;DR: Rongalite as a novel precursor of super electron donors was used to initiate a series of electron-catalyzed reactions under mild conditions that enable the efficient formation of C-C, C-S and C-P bond through homolytic aromatic substitution or SRN1 reactions.
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Process for preparing quetiapine fumarate
TL;DR: In this article, a novel synthesis of quetiapine, and pharmaceutically acceptable salts thereof, in which an alkali metal halide or siliyl halide is included in the reaction mixture is provided.
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A process for the preparation of quetiapine
TL;DR: In this article, a method for the preparation of 11- (4- [2- hydroxyethoxy) ethyl] -1-piperazinyl] dibenzo [b, f ] -1, 4-thiazepine and pharmaceutically acceptable salts thereof was described.
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Improved process for preparing quetiapine fumarate
TL;DR: In this article, an improved synthesis of quetiapine and pharmaceutically acceptable salts using a compound of formula [III] wherein A is chlorine, bromine or iodine which is formed by reaction of a compound with a halogenating agent and an aliphatic halogenated hydrocarbon in the absence of a base.
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Process for the preparation of quetiapine fumarate
Venugopal Venkatarama Durvasula,Parendu Dhirajlal Rathod,Ram Chandra Aryan,Chandra Has Khanduri +3 more
TL;DR: In this paper, an improved process for the preparation of quetiapine and pharmaceutically acceptable salts was presented, and the improved process was used for the synthesis of intermediates of queto-apine.
References
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New (sulfonyloxy)piperazinyldibenzazepines as potential atypical antipsychotics: chemistry and pharmacological evaluation.
Yi Liao,Bastiaan J. Venhuis,Nienke Rodenhuis,W Timmerman,Hakan Wikstrom,Eddie Meier,Gerd Bartoszyk,Henning Böttcher,Christoph Seyfried,S. Sundell +9 more
TL;DR: The 2-TfO analogues of 11-piperazinyldibenzazepines are promising candidates as clozapine-like atypical antipsychotics with low propensity to induce EPS.
Patent
Process for the preparation of a thiazepine compound
TL;DR: In this paper, 11-piperazinyldibenzo[b,f][1,4]thiazepine and the salts thereof possess anti-andropaninergic activity.
Patent
NEW SULFONE ESTER ANALOGUES OF iso-CLOZAPINE AND RELATED STRUCTURES: ATYPICAL NEUROLEPTICS
TL;DR: A compound of formula (I), or pharmaceutically acceptable acid addition salts thereof, wherein R1 is H, (C1-C8) alkyl or haloalkyl or hydroxyalkyl, alkenyl, alkynyl, cyclopropylalkyl and X is NH, NR1, O, S, SO, SO2 as discussed by the authors.