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13745-86-3Relevant academic research and scientific papers
Synthesis of diverse fused tetracyclic thiazepine-chalcone derivatives by claisen-schmidt condensation reaction and their antimicrobial activity
Hirani, Jayanti B.,Pandya, Mayank K.,Koradiya, Suresh B.
, p. 2860 - 2864 (2020)
To develop antimicrobial agent, a series of thiazepine-chalcones was synthesized by Claisen-Schmidt condensation between the couplings of aryl ketone in three steps protocol and different aromatic aldehydes under strong base catalyst at room temperature. The characterization of final products were carried out by IR, 1H & 13C NMR and elemental analysis. The synthesized compounds were also evaluated for their antibacterial and antifungal activities using specific Gram positive and Gram-negative bacterial strains using cup plate method.
Design of Conjugated Molecules Presenting Short-Wavelength Luminescence by Utilizing Heavier Atoms of the Same Element Group
Yamaguchi, Madoka,Tanaka, Kazuo,Chujo, Yoshiki
, p. 1342 - 1347 (2018)
The introduction of heavy atoms into conjugated molecules often induces a redshift in the emission spectra. Conversely, we report here a blueshifting effect in the absorption and emission bands of a conjugated organic dye by employing a heavier atom from the same element group. Boron complexes having oxygen- and sulfur-bridged structures in the ligand moiety were synthesized, and their optical properties were compared. Significant optical bands in the absorption and luminescence spectra of the sulfur-bridged complex were observed in a shorter wavelength region than those of the oxygen-bridged complex. Theoretical calculations suggest that replacement of the bridging atom by a heavier one should reduce molecular planarity because of the larger atom size. As a result, the degree of electronic conjugation decreases, and this is followed by a blueshift in the optical bands. Finally, a blue-emissive crystal is demonstrated.
INFLUENZA VIRUS REPLICATION INHIBITOR AND USE THEREOF
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Paragraph 0274; 0278, (2020/08/09)
Disclosed are a compound as shown in formula (I) as an influenza virus replication inhibitor and a preparation method therefor, a pharmaceutical composition comprising the compound and the use of the compound and pharmaceutical composition thereof in the treatment of influenza.
Preparation method of quetiapine fumarate intermediate
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Paragraph 0031-0049, (2019/04/26)
The invention discloses a preparation method of a quetiapine fumarate intermediate. The method comprises the following steps: taking 10,11-dihydro-11-oxodibenzo[b,f][1,4]thiazepine and oxalyl chlorideas raw materials to prepare 11-chloro-dibenzo[b,f][1,4]thiazepine in an anhydrous organic solvent under the combined action of 4-substituted pyridine and pyridine, wherein the purity of the product is larger than or equal to 97.0%, and the yield is larger than or equal to 90%. The method has mild reaction conditions, good environmental protection performance and a high product yield, and is easyfor industrial production.
Antibodies to quetiapine haptens and use thereof
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, (2018/01/20)
Disclosed is an antibody which binds to quetiapine, which can be used to detect quetiapine in a sample such as in a competitive immunoassay method. The antibody can be used in a lateral flow assay device for point-of-care detection of quetiapine, including multiplex detection of aripiprazole, olanzapine, quetiapine, and risperidone in a single lateral flow assay device.
Methods for Treating Cognitive Disorders Using Inhibitors of Histone Deacetylase
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Paragraph 0413; 0444, (2017/01/23)
This disclosure relates to compounds for the inhibition of histone deacetylase and treatment of a cognitive disorder or deficit. More particularly, the disclosure provides for compounds of formula (I) wherein Q, J, L and Z are as defined in the specification.
Design, synthesis and anticancer activity of N-(1-(4-(dibenzo[b,f][1,4]thiazepin-11-yl)piperazin-1-yl)-1-oxo-3-phenylpropan-2-yl derivatives
Gudisela, Mura Reddy,Srinivasu,Mulakayala, Chaitanya,Bommu, Praveen,Rao, M.V. Basaveswara,Mulakayala, Naveen
, p. 4140 - 4145 (2017/08/23)
Novel N-(1-(4-(dibenzo[b,f][1,4]thiazepin-11-yl)piperazin-1-yl)-1-oxo-3-phenylpropan-2-yl derivatives were designed, synthesized and their chemical structures were confirmed by 1H NMR, 13C NMR and Mass spectra. The anticancer activities of the newly synthesized compounds were evaluated in vitro against three human cancer cell lines including K562, Colo-205 and MDA-MB 231 by MTT assay. The screening results showed that five compounds (16b, 16d, 16i, 16p and 16q) exhibited potent cytotoxic activities with IC50 values between 20 and 40 μM. Further in vitro studies revealed that inhibition of sirtuins could be the possible mechanism of action of these molecules.
Quetiapine synthesizing method
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, (2017/06/27)
The invention discloses a quetiapine synthesizing method. O-chlorobenzoic acid with the low price is adopted as a starting material to react with thiophenol, and then ring closure is performed to obtain thioxanthone. Hydroxyl amination and Beckmann rearrangement are performed to obtain a key intermediate dibenzo[b,f][1,4]thiazepines-11-(10H)one, chlorination is performed, then, a reaction is performed on 1-(2-hydroxyethoxy)ethylpiperazine with the existence of acid-binding agent to obtain quetiapine, and the quetiapine and fumaric acid form a salt in an absolute ethyl alcohol system to obtain a product. According to the quetiapine synthesizing method, raw materials are low in price and easy to obtain, the steps are simple, operation is easy, and the cost can be effectively lowered. According to the method, the high-purity quetiapine can be obtained, the liquid phase purity of the obtained semi-fumaric acid quetiapine obtained through salt forming is 99% or above, and the quetiapine synthesizing method can be applied to the field of medicine.
A Vilsmeier reagent in the 11- chlorine benzoin and [b, f] [1,4] preparation method of allowing to sulfur, nitrogen
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Paragraph 0018-0019, (2017/01/17)
The invention discloses a preparation method of 11-chlorodibenzo[b,f][1,4]thiazepine in presence of a Vilsmeier reagent. The preparation method comprises the following steps: by using 10H-dibenzo[b,f][1,4]thiazepine-11-one as shown in a structural formula (I) and the Vilsmeier reagent as shown in a structural formula (III) as raw materials, preparing the 11-chlorodibenzo[b,f][1,4]thiazepine as shown in the structural formula (II) through a heating reaction in an organic solvent, wherein the Vilsmeier reagent is prepared from di-(trichloromethyl)carbonic ester as shown in a structural formula (a) and DMF (Di-Methyl Formamide) as shown in a structural formula (b). The preparation method provided by the invention has the advantages of short reaction time, simplicity and convenience in operation, simple post-treatment, less pollution and low cost and the like and is a chemical synthesis method with a better popularization and application prospect.
Pyrophosphoryl Chloride: A Green, Reductive Chlorination Reagent Utilized in the One-Pot Synthesis of Quetiapine
Mahmoodi,Pourhossein Parizad,Hosseini
, p. 1029 - 1034 (2015/08/04)
A one-pot synthesis of quetiapine from dibenzo[b,f][1,4]thiazepin-11(10H)-one and 4-hydroxyethoxy ethyl piperazine (HEEP) in toluene using N,N-dimethylaniline (DMA) and pyrophosphoryl chloride (P2O3Cl4) as a green reductive chlorination agent is described. A significant shortening of reaction times, a nearly quantitative yield, and high atom economy in the product were observed. The simplicity of the reaction, ease of execution, simple workup, and good yields, together with the use of easily accessible starting materials and an environmentally friendly procedure, are hallmarks of this process.
