Showing papers on "Thiazepine published in 2015"
TL;DR: A two-step diversity oriented synthetic protocol to a novel class of dihydrodibenzo-11-carboxamides has been developed and ensures the synthesis of dibenzothiazepine via copper-mediated condition followed by Ugi–Joullie reaction of the resultant cyclic imine.
Abstract: A two-step diversity oriented synthetic protocol to a novel class of dihydrodibenzo[b,f][1,4]thiazepine-11-carboxamides has been developed. The first step ensures the synthesis of dibenzothiazepine via copper-mediated condition followed by Ugi–Joullie reaction of the resultant cyclic imine in the second step.
28 citations
TL;DR: This study involved, synthesis of new sulfur organic compounds, the important class of heterocyclic and exhibits a wide range of biological properties and due to its potent and significant pharmacological activities.
Abstract: This study involved, synthesis of new sulfur organic compounds like Thiazole, Thiadiazole, Thiazine, Thiadiazine, Thiazepine and Thiadiazepin (heterocyclic compounds), the important class of heterocyclic and exhibits a wide range of biological properties and due to its potent and significant pharmacological activities. All steps of reactions followed by TLC-papers. All the synthesized compounds have been investigated using different chemical techniques, such as (1H.NMR-spectra, (C.H.N)-analysis, FT.IR-spectra) ome of them in 13C.NMR-spectra, melting points and biological study.
20 citations
TL;DR: Several derivatives of the novel dihydrobenzo[b]pyrimido[4,5-e][1,4]thiazepine ring system have been synthesised through the initial heterocyclisation of 2,4-dichloro-5-(chloromethyl)-6-methylpyrim...
Abstract: Several derivatives of the novel dihydrobenzo[b]pyrimido[4,5-e][1,4]thiazepine ring system have been synthesised through the initial heterocyclisation of 2,4-dichloro-5-(chloromethyl)-6-methylpyrim...
12 citations
TL;DR: A mild and efficient synthesis of pyrazolo[3,4-e][1,4]thiazepine derivatives through an l-proline catalyzed multi-component reaction is developed and almost all the compounds were found to exhibit good to moderate activity.
Abstract: Herein, we have developed a mild and efficient synthesis of pyrazolo[3,4-e][1,4]thiazepine derivatives through an l-proline catalyzed multi-component reaction. The synthesized compounds were subjected to in vitro cytotoxicity studies toward pancreas (PANC1), renal (ACHN) and colon (HCT116), non-small cell lung (H460), lung (CALU1), and normal breast epithelium (MCF10A) cell lines and almost all the compounds were found to exhibit good to moderate activity. The compounds 4a, 4d, 4f, 4h, and 4k were found to possess prominent cytotoxic activity toward all cell lines tested. Of the compounds tested, 4f and 4k were found to possess activity equal to the control used toward all tested cell lines with 52.7–80.6 % GI values.
7 citations
TL;DR: For the first time, thermally induced ring transformation and expansion of triarylthiopyrylium salts using a novel task-specific dicationic ionic liquid [1,1′-(butane-1,4-diyl)-b... was reported in this paper.
Abstract: The paper reports, for the first time, thermally induced ring transformation and expansion of triarylthiopyrylium salts using a novel task-specific dicationic ionic liquid [1,1′-(butane-1,4-diyl)-b...
5 citations
TL;DR: Conditions A) are highly suitable for the preparation of various ring-opened addition products, precursors of the desired benzoxazepine and benzothiazepine structures as mentioned in this paper.
Abstract: Conditions A) are highly suitable for the preparation of various ring-opened addition products, precursors of the desired benzoxazepine and benzothiazepine structures.
1 citations
Patent•
29 Jul 2015
TL;DR: In this article, a preparation method of 11-(1-piperazinyl) dibenzo[b, f][1,4] thiazepine fumarate was proposed.
Abstract: The invention relates to a preparation method of 11-(1-piperazinyl) dibenzo[b, f][1,4] thiazepine fumarate. The preparation method comprises steps as follows: 2-(2-nitro-thiophenyl)-benzoic acid(I) has a chlorination reaction firstly to generate 2-(2-nitro-thiophenyl)-benzoyl chloride (II); the compound II reacts with piperazine in the presence of an acid binding agent to generate piperazinyl-[2-(2-nitro) thiophenyl] benzophenone(III); the nitro group of the compound III is reduced to an amino group through a hydrogenation reaction, and piperazinyl-[2-(2-amino)-thiophenyl]-benzophenone(IV) is obtained; in xylene, tetraisopropyl titanate is taken as a condensation agent, the compound IV has a cyclization reaction to generate 11-(1-piperazinyl) dibenzo[b, f][1,4] thiazepine; 11-(1-piperazinyl) dibenzo[b, f][1,4] thiazepine and fumaric acid have a salt forming reaction to obtain 11-(1-piperazinyl) dibenzo[b, f][1,4] thiazepine fumarate. The preparation method has the benefits as follows: phosphorus reagents are not used, column chromatography purification is not required, the purity of 11-(1-piperazinyl) dibenzo[b, f][1,4] thiazepine fumarate is higher than 99.0%, and quetiapine can be obtained through a one-step reaction.
1 citations
TL;DR: A new series of 4-(2'-oxo/thiobarbiturinyl)-2-(substitutedphenyl)-3-[(substitized aminomethylene)]-2,3-dihydro-1, 5benzoxazepines (6a-6l) were synthesized.
Abstract: A new series of 4-(2'-Oxo/thiobarbiturinyl)-2-(substitutedphenyl)-3-[(substituted aminomethylene)]-2,3-dihydro-1,5-benzothiazepines (5a-5l) and 4-(2'-oxo/thiobarbiturinyl)-2(substituted-phenyl)-3-(substitutedaminomethylene)]-2,3-dihydro-1, 5benzoxazepines (6a-6l) were synthesized. All the newly synthesized compounds were screened in vivo, for their acute toxicity and anticonvulsant activity in MES and PTZ models and were compared with standard drugs phenytoin sodium and sodium valporate. Out of the compounds studied, the most active compound of this series was 5h, showed activity (90%) more potent than the standard drug.
1 citations
Patent•
25 Nov 2015
TL;DR: In this article, a preparation method for a crystalline dibenzothiazepine derivative is presented, which is synthesized through chlorination reaction, condensation reaction and salt forming reaction by taking dibenzo[b,f][1,4]thiazepine-11-[10H]one as an initial raw material.
Abstract: The invention discloses a preparation method for a crystalline dibenzothiazepine derivative. The crystalline dibenzothiazepine derivative is synthesized through chlorination reaction, condensation reaction and salt forming reaction by taking dibenzo[b,f][1,4]thiazepine-11-[10H]one as an initial raw material. According to the preparation method, in preparation of 11-chlorine-dibenzo[b,f][1,4]thiazepine, phosphorus oxychloride which is high in toxicity and pollution is replaced by oxalyl chloride which is low in toxicity and pollution; the use of N,N-dimethyl aniline which is high in pollution is prevented, so that the pollution on the environment is greatly reduced; by virtue of salification by crystalline 11-[4-[2-(2-hydroxyl ethoxyl)ethyl]-1-piperazinyl]dibenzo[b,f][1,4]thiazepine free alkali, acquisition of high quality fumarate is ensured, the production cost is effectively lowered, and the batch production is facilitated.
1 citations
TL;DR: In this article, the thiazepine carboxamides (VI) were obtained by a two-step diversity oriented synthetic method including the copper-catalyzed synthesis of dibenzothiazepine as first step followed by Ugi-Joulli reaction of the obtained cyclic imines as second step.
Abstract: The thiazepine carboxamides (VI) are obtained by a two-step diversity oriented synthetic method including the copper-catalyzed synthesis of dibenzothiazepine as first step followed by Ugi—Joulli reaction of the obtained cyclic imines as second step.
Patent•
12 Mar 2015
TL;DR: The preparation method has the benefits as follows: phosphorus reagents are not used, column chromatography purification is not required, the purity of 11-(1-piperazinyl) dibenzo[b, f][1,4] thiazepine fumarate is higher than 99.0%, and quetiapine can be obtained through a one-step reaction.
Abstract: The invention relates to a preparation method of 11-(1-piperazinyl) dibenzo[b, f][1,4] thiazepine fumarate. The preparation method comprises steps as follows: 2-(2-nitro-thiophenyl)-benzoic acid(I) has a chlorination reaction firstly to generate 2-(2-nitro-thiophenyl)-benzoyl chloride (II); the compound II reacts with piperazine in the presence of an acid binding agent to generate piperazinyl-[2-(2-nitro) thiophenyl] benzophenone(III); the nitro group of the compound III is reduced to an amino group through a hydrogenation reaction, and piperazinyl-[2-(2-amino)-thiophenyl]-benzophenone(IV) is obtained; in xylene, tetraisopropyl titanate is taken as a condensation agent, the compound IV has a cyclization reaction to generate 11-(1-piperazinyl) dibenzo[b, f][1,4] thiazepine; 11-(1-piperazinyl) dibenzo[b, f][1,4] thiazepine and fumaric acid have a salt forming reaction to obtain 11-(1-piperazinyl) dibenzo[b, f][1,4] thiazepine fumarate. The preparation method has the benefits as follows: phosphorus reagents are not used, column chromatography purification is not required, the purity of 11-(1-piperazinyl) dibenzo[b, f][1,4] thiazepine fumarate is higher than 99.0%, and quetiapine can be obtained through a one-step reaction.
TL;DR: In this article, the reaction between o-aminothiophenol and 4-(2-furyl)-3-nitrobut-3-en-2-one affords 4methyl-3 -nitro-2-(2)-furyls)-2,5 -dihydro-1,5-benzo- thiazepine whose structure was characterized by X-ray diffraction analysis.
Abstract: Reaction between o-aminothiophenol and 4-(2-furyl)-3-nitrobut-3-en-2-one affords 4-methyl-3-nitro-2-(2-furyl)-2,5-dihydro-1,5-benzo- thiazepine whose structure was characterized by X-ray diffraction analysis.