Showing papers on "Thiazepine published in 2002"
TL;DR: In this article, the synthesis of new thiazepine compounds bearing a non substituted sulfonamide group was described through two different synthetic pathways, which were used to design new anticancer structural families.
4 citations
Patent•
27 Aug 2002
TL;DR: In this article, a process for the industrial synthesis of the compound of formula (I): and its addition salts is described.Application to the synthesis of tianeptine and its pharmaceutically acceptable salts.
Abstract: Process for the industrial synthesis of the compound of formula (I): and its addition salts.Application to the synthesis of tianeptine and its pharmaceutically acceptable salts.
4 citations
TL;DR: In this article, the 13C NMR spectra of 2-phenyl- and 2-benzyliminohexahydro-1,3-thiazepines were studied.
Abstract: We have studied the 13C NMR spectra of 2-phenyl- and 2-benzyliminohexahydro-1,3-thiazepines, and also their alkyl, acyl, carbamoyl, and thiocarbamoyl derivatives We have shown that introducing substiuents both into the 2 position and into the 3 position of the thiazepine ring mainly affects the chemical shifts for the C(4) of the heterocycle
1 citations
TL;DR: In this article, a methodology directed toward the stereoselective synthesis of novel quinolyl glycines is presented, which is based on the cyclocondensation reaction between 2-amino thiophenol 4 and chiral acetylenic ketones of the type 3 containing a latent αamino acid functionality.
Abstract: A methodology directed toward the stereoselective synthesis of novel quinolyl glycines is presented. This strategy is based on the cyclocondensation reaction between 2-amino thiophenol 4 and chiral acetylenic ketones of the type 3 containing a latent α-amino acid functionality. The initially formed benzo[b][1,4]thiazepine derivatives 5, readily undergo sulphur extrusion in refluxing toluene to yield the corresponding 2,4-disubstituted quinolines 6. Subsequent oxazolidine ring opening followed by in situ re-protection of the amino group afforded the corresponding quinolyl-β-amino alcohols 8a–8f in enantiomerically pure form and good overall yields. The derivatives 8 are in principle suitable precursors for the synthesis of novel optically pure quinolyl glycines through oxidation of the alcohol side chain. However, these amino alcohol derivatives 8, did not afford the expected quinolyl glycines 10 using numerous oxidising agents and reaction conditions. Instead, by reacting 8 with the mild oxidising reagent IBX 11, an oxidative CC cleavage leading to the N-Boc quinolyl carboxamides 12 took place.
1 citations
Patent•
16 Oct 2002
TL;DR: In this paper, a novel process for the preparation of 11-[4/2-(2-hydroxyethoxy)ethyl/-1-piperazinyl]dibenzo[b,f]-1,4-thiazepine of the general formula I known as quetiapine was described.
Abstract: The present invention relates to a novel process for the preparation of 11-[4-/2-(2-hydroxyethoxy)ethyl/-1-piperazinyl]dibenzo[b,f]-1,4-thiazepine of the general formula I known as quetiapine. According to the invention, a haloethyl piperazinyl thiazepine derivative of the general formula VIII, wherein Hal stands for a halo atom, is reacted with ethylene glycol.