cas 3159-07-7, 10,11-Dihydro-11-oxodibenzo[b,f][1,4]thiazepine

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The behaviour of some thioxanthene and thianthrene derivatives with hydrazoic acid
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Palazzo,Giannola,Caronna
p. 839 - 841
(1974)
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Photoisomerization of 2-Aryl-1,2-benzisothiazol-3(2H)-ones
Photoisomerization of the benzisothiazol-3(2H)-ones (1) gives the dibenzothiazepin-10(11H)-ones (4) probably via homolytic cleavage of the S-N bond (2)>, cyclization of the biradical (3)>, followed by the formation of an aromatic ring together with 1,7 hydrogen transfer (4)>.
Kamigata, Nobumasa,Hashimoto, Satoshi,Fujie, Shin-ichi,Kobayashi, Michio
p. 765 - 766
(1983)
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Diversity in Heterocycle Synthesis Using α-Iminocarboxylic Acids: Decarboxylation Dichotomy
Despite the structural similarity with imines, α-iminocarboxylic acids have seldom been used in heterocycles synthesis. The reactions of ortho-substituted anilines and arylglyoxylic acids in DMSO at 40 °C gave various benzo-fused five- to six-membered N-heterocycles in good to excellent yields. The reaction proceeds via intramolecular Michael addition of α-iminocarboxylic acids, generated in situ, with an ortho-substituted nucleophile, yielding an isolable unprecedented tetrahedral carboxylic acids, which upon decarboxylation without any aid of additional reagents forms the N-heterocycles. DMSO is crucial in this reaction, perhaps because of improved solubility and the ease of decarboxylation of these tetrahedral carboxylic acids. However, a copper-catalyzed reaction of ortho-substituted anilines and 2-bromoarylglyoxylic acids gave a dibenzo-fused seven-membered N-heterocycle under a basic reaction condition. Unlike intramolecular cyclization with α-iminocarboxylic acids in the first case, α-iminocarboxylic acid undergoes a competitive decarboxylation under the copper-catalyzed conditions, which upon subsequent heteroarylation form the heterocycles. Taken together, the study described herein represents two different modes of decarboxylation observed with α-iminocarboxylic acids, leading to the synthesis of divergent heterocycles and pharmaceuticals, which remained unexplored previously.
Laha, Joydev K.,Hunjan, Mandeep Kaur
p. 2315 - 2323
(2022/02/07)

INFLUENZA VIRUS REPLICATION INHIBITOR AND USE THEREOF
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.
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(2020/08/09)

Reductive Condensation of a Nitro Group with Carboxylic Acids Promoted by Phosphorus(III) Compounds: A Short Route to 5 H -Dibenzo[ b, e ][1,4]diazepin-11(10 H)-ones
Tributyl- or triphenylphosphine promotes a one-pot, three-step method for the synthesis of differently substituted dibenzodiazepinones from N -aryl-2-nitroanilines. Pyridine analogues and the corresponding thiazepinones can also be formed using this method. The process involves deoxygenation of the nitro group, then formation of an iminophosphorane intermediate and its intramolecular condensation with a carboxyl group placed in the N -aryl group. The role of the carboxyl group in the formation of the iminophosphorane and the mode of cyclization are discussed.
Tryniszewski, Micha?,Bujok, Robert,Gańczarczyk, Roman,Wróbel, Zbigniew
p. 3086 - 3094
(2020/08/10)

Design, synthesis, and molecular docking study of new piperazine derivative as potential antimicrobial agents
Herein, we describe the successful design and synthesis of seventeen new 1,4-diazinanes, compounds commonly known as piperazines. This group of piperazine derivatives (3a-q) were fully characterized by 1H NMR, 13C NMR, FT-IR, and LCMS spectral techniques. The molecular structure of piperazine derivative (3h) was further established by single crystal X-ray diffraction analysis. All reported compounds were evaluated for their antibacterial and antifungal potential against five bacterial (Staphylococcus aureus, Escherichia coli, Klebsiella pneumoniae, Acinetobacter baumannii, and Pseudomonas aeruginosa) and two fungal strains (Candida albicans and Cryptococcus neoformans). The complete bacterial screening results are provided. As documented, piperazine derivative 3e performed the best against these bacteria. Additionally, data obtained during molecular docking studies are very encouraging with respect to potential utilization of these compounds to help overcome microbe resistance to pharmaceutical drugs, as explicitly noted in this manuscript.
Patil, Mahadev,Noonikara Poyil, Anurag,Joshi, Shrinivas D.,Patil, Shivaputra A.,Patil, Siddappa A.,Bugarin, Alejandro
supporting information

(2019/09/06)

COtab: Expedient and Safe Setup for Pd-Catalyzed Carbonylation Chemistry
Bench-stable tablets (COtabs) have been developed for the rapid and safe production of carbon monoxide. The tablets can be made in less than 5 min without the use of a glovebox and only require a stock solution of an amine base to liberate a specific quantity of CO in a two-chamber system. The COtabs were tested in five different carbonylation reactions and provided similar yields compared to literature procedures. Finally, a gram-scale reaction was conducted, as well as 13C-isotope labeling of the anticancer drug, olaparib.
Collin, Hugo P.,Reis, Wallace J.,Nielsen, Dennis U.,Lindhardt, Anders T.,Valle, Marcelo S.,Freitas, Rossimiriam P.,Skrydstrup, Troels
supporting information
p. 5775 - 5778
(2019/08/26)

Generation of Aryl Radicals from Aryl Halides: Rongalite-Promoted Transition-Metal-Free Arylation
A new and practical method for the generation of aryl radicals from aryl halides is reported. Rongalite as a novel precursor of super electron donors was used to initiate a series of electron-catalyzed reactions under mild conditions. These transition-metal-free radical chain reactions enable the efficient formation of C-C, C-S, and C-P bonds through homolytic aromatic substitution or SRN1 reactions. Moreover, the synthesis of antipsychotic drug Quetiapine was performed on gram scale through the described method. This protocol demonstrated its potential as a promising arylation method in organic synthesis.
Yu, Fazhi,Mao, Runyu,Yu, Mingcheng,Gu, Xianfeng,Wang, Yonghui
supporting information
p. 9946 - 9956
(2019/09/04)

Cobalt-Catalyzed Direct C-H Thiolation of Aromatic Amides with Disulfides: Application to the Synthesis of Quetiapine
A direct C(sp2)-H thiolation of aromatic amides with disulfides was developed. The coupling reaction proceeds between the thioether radical and cobaltacycle intermediate. This method exhibits a relatively broad substrate scope and high functional group compatibility. A mechanistic study indicates that the cobalt(IV) intermediate is probably formed during the course of the reaction. The thiolation product can be transformed to Quetiapine, which is an atypical antipsychotic agent approved for the treatment of schizophrenia and bipolar disorder.
Li, Mingliang,Wang, Jun Joelle
p. 6490 - 6493
(2018/10/20)

Antibodies to quetiapine haptens and use thereof
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.
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Page/Page column 41-42

(2018/01/20)

Ligand-Controlled Chemoselective One-Pot Synthesis of Dibenzothiazepinones and Dibenzoxazepinones via Twice Copper-Catalyzed Cross-Coupling
A highly efficient and generally applicable protocol, starting from 2-bromobenzamides and 2-bromo(thio)phenols via twice copper-catalyzed couplings to afford dibenzothiazepines and dibenzoxazepinones has been developed. High levels of yield and chemoselectivity are achieved in a single-pot reaction by using an appropriate ligand. Moreover, this facile methodology allows rapid access to a variety of bio-active compounds and known psychotropic drug, which should broaden its application in organic synthesis.
Chen, Yanyu,Peng, Qiujun,Zhang, Rong,Hu, Jian,Zhou, Yijun,Xu, Lanting,Pan, Xianhua
supporting information
p. 1201 - 1208
(2017/06/14)

Methods for Treating Cognitive Disorders Using Inhibitors of Histone Deacetylase
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.
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(2017/01/23)

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
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.
Gudisela, Mura Reddy,Srinivasu,Mulakayala, Chaitanya,Bommu, Praveen,Rao, M.V. Basaveswara,Mulakayala, Naveen
p. 4140 - 4145
(2017/08/23)

Quetiapine synthesizing method
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.
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Paragraph 0071; 0072

(2017/06/27)

A process for the preparation of intermediates quetiapine (by machine translation)
The invention discloses a preparation method for a quetiapine intermediate. The preparation method comprises: taking thiosalicylic acid as an initial raw material to prepare 2-nitro-2'-carboxyldiphenyl sulfide, esterifying and reducing, and then performing intramolecular amino-ester exchange reaction for cyclization, so as to obtain the quetiapine intermediate 10,11-dihydro-11-oxodibenzo[b,f][1,4]thiazepine. The preparation method is simple, the target product is high in purity, the reaction yield is relatively high, the production cost is effectively reduced, and industrialized production of the high-purity quetiapine intermediate is facilitated to be realized.
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Paragraph 0022

(2017/02/24)

A method for preparing [...]
The invention discloses a preparation method of quetiapine hemifumarate. The preparation method of quetiapine hemifumarate comprises the following steps: etherifying, hydrogenating, condensing and carrying out chlorination by taking o-chloronitrobenzene and thiophenol as raw materials, and finally salifying with fumaric acid, thereby obtaining quetiapine hemifumarate. The production technology is simple to operate and convenient for large-scale production, the cost is saved and the high-purity high-yield quetiapine hemifumarate can be obtained.
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Paragraph 0037

(2017/03/14)

Preparation 10H-dibenz [b, f] [1,4] parathiazine -11-ketone and method of quetiapine
The invention provides a method for synthesizing a quetiapine mother-ring intermediate, and the method comprises the following steps: esterification of 2-nitro - 2'-carboxyl diphenyl sulfide, and under the right conditions, nitroreduction simultaneously with ester aminolysis to obtain the product 10 H-dibenzo[b,f][1,4]thiazepin-11-one and quetiapine by a one pot method. Compared with a traditional method, the method has the advantages of being simple in operation, high in yield, more suitable for industrial production, and the like.
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Paragraph 0050; 0051

(2017/03/08)

Discovery of Novel Tricyclic Thiazepine Derivatives as Anti-Drug-Resistant Cancer Agents by Combining Diversity-Oriented Synthesis and Converging Screening Approach
An efficient discovery strategy by combining diversity-oriented synthesis and converging cellular screening is described. By a three-round screening process, we identified novel tricyclic pyrido[2,3-b][1,4]benzothiazepines showing potent inhibitory activity against paclitaxel-resistant cell line H460TaxR (EC50 50 > 100 μM against normal human fibroblasts). The most active hits also exhibited drug-like properties suitable for further preclinical research. This redeployment of antidepressing compounds for anticancer applications provides promising future prospects for treating drug-resistant tumors with fewer side effects.
Xiang, Jinbao,Zhang, Zhuoqi,Mu, Yan,Xu, Xianxiu,Guo, Sigen,Liu, Yongjin,Russo, Daniel P.,Zhu, Hao,Yan, Bing,Bai, Xu
supporting information
p. 230 - 235
(2016/06/01)

Antibodies to Quetiapine Haptens and Use Thereof
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.
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(2014/03/24)

HAPTENS OF QUETIAPINE FOR USE IN IMMUNOASSAYS
The invention relates to compounds of Formula I, wherein R1, R2, and R3 are defined in the specification, useful for the synthesis of novel conjugates and immunogens derived from quetiapine. The invention also relates to conjugates of a quetiapine hapten and a protein.
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Page/Page column 56

(2014/03/25)

Synthesis, characterization and antimicrobial activity of 2-(11-oxodibenzo [b,f][1,4]thiazepin-10(11H)-yl)-N (substituted phenyl) acetamide derivatives
Substituted dibenzo [b,f][1,4]thiazepines analogues carrying 2-chloro N-phenylacetamide moiety attached to 11-C position have been synthesized and evaluated using IR, 1H NMR and mass spectra. Antibacterial properties have been examined for the synthesized derivatives against gram positive and gram negative bacteria. 2-(11-Oxodibenzo [b,f][1,4]thiazepin-10(11H)-yl)-N phenylacetamide derivatives show good significant antimicrobial activity.
Tailor, Jitesh H.,Patel, Priti C.,Malik
p. 1263 - 1268
(2014/12/10)

Diversified synthesis of novel quinoline and dibenzo thiazepine derivatives using known active intermediates
The novel drug development to control resisting infections in conventional drug therapy is a need of today. Few antiulcer relative derivatives developed by approaching convergent synthesis. The derivatives synthesized successfully are dibenzo thiazepine-pyridine (SLN11-SLN15) and benzimidazole-hydroquinoline based derivatives (SLN16-SLN20). It involved the coupling through microwave, sonication and conventional techniques at final step. The efficient technology identified as sonication technique basically time and yield. The reported compounds were structural characterized by elemental analysis and spectral studies such as 1H, 13C NMR and MS.
Sharada,Satyanarayana Reddy,Sammaiah,Sumalatha
p. 7959 - 7966
(2013/09/23)

Heterogeneous magnetic catalyst for S-arylation reactions
A convenient method for the synthesis of monodisperse, superparamagnetic copper ferrite (CuFe2O4) nanoparticles with high surface area has been described. The synthesized material was characterized by various techniques. XRD showed the nanocrystalline nature of CuFe2O 4 with a crystallite size of 6 nm. TEM analysis showed that uniform spherical CuFe2O4 particles are formed with a size of 55 ± 5 nm. N2 adsorption/desorption measurements confirmed the mesoporous nature of the sample with surface area >216 m2 g -1. The field dependent magnetization, illustrated by VSM and saturation magnetization was found to be 44 emu g-1. The catalytic applications of the synthesized CuFe2O4 nanoparticles were explored for the cross-coupling of thiols with diverse range of aryl halides. Aryl iodides and bromides result in biarylsulfides in good to excellent yields (62-98%) whereas aryl chlorides gave significant amount of diaryldisulfide. Scope of this catalytic protocol further extended to one-pot synthesis of biologically important tricyclic dibenzothiazepines. The superparamagnetic nature of CuFe2O4 nanoparticles was found to be advantageous for their easy, quick and quantitative separation from the reaction mixture. Negligible leaching of Cu and Fe in consecutive cycles makes the catalyst economical and environmentally benign.
Panda, Niranjan,Jena, Ashis Kumar,Mohapatra, Sasmita
experimental part
p. 258 - 264
(2012/08/28)

Synthesis and antibacterial activities of new dibenzothiazepine derivatives
A number of substituted dibenzo[b,f][1,4]thiazepines analogues carrying heterocyclic and aliphatic moiety attached to C-11 position have been synthesized and evaluated their antibacterial activities against gram positive and gram negative bacteria. Derivatives of imidazole, 2-methyl imidazole and pyrrolidine exhibit significant antibacterial activities.
Mahale, Ganesh D.,Kolekar, Yogesh M.,Kumar, Ashok,Singh, Dharmendra,Kodam, Kisan M.,Waghmode, Suresh B.
p. 1196 - 1201
(2011/10/12)

PROCESS FOR PREPARATION OF DIBENZOTHIAZEPINONE COMPOUNDS
The present invention discloses a process for the preparation of dibenzothiazepinone compounds of Formula I. The process for preparation of a dibenzothiazepinone compound of Formula I comprises reaction of compound of formula II in the presence of an acid catalyst comprising phosphorus pentoxide and methanesulfonic acid. The dibenzothiazepinone compounds of Formula I are key intermediate for the preparation of 2-(2-(4-dibenzo[b,f][1,4]thiazepine-11-yl-1-piperazinyl)ethoxy)ethanol known as quetiapine and its derivatives, which are effective antipsychotic substances.
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Page/Page column 9-10

(2011/10/13)

Process for preparing dibenzothiazepine compounds
A dibenzothiazepine compound is suitably prepared by subjecting a 2-amino-2′-carboxy-diphenylsulfide compound to dehydration-condensation reaction in the presence of an acidic catalyst; the 2-amino-2′-carboxy-diphenylsulfide compound is suitably prepared by reducing a 2-nitro-2′-carboxy-diphenylsulfide compound in a lower aliphatic ester solvent; and the 2-nitro-2′-carboxy-diphenylsulfide compound is suitably prepared by reacting a nitrobenzene compound with a thiosalicylic acid compound in a mixture of a lower aliphatic alcohol and water.
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Page/Page column 7

(2008/06/13)

IRON CATALYZED CROSS-COUPLING REACTIONS OF IMIDOYL DERIVATIVES
Disclosed is a process for preparing a compound of formula A - N=C(D)(B), from a compound of formula A-N=C(E)(B) and a compound of formula D-M using an iron catalyst, where the process has is represented by Equation (I).
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Page/Page column 21; 52

(2010/11/27)

SUBSTITUTED PIPERAZINES OF AZEPINES, OXAZEPINES, AND THIAZEPINES
Described herein are antipyschotic compounds of formula (I) wherein: is an optionally benzo-fused five or six member aromatic ring having zero to three hetero atoms independently selected from N, O, and S; R1 is hydrogen, (C1-6) fluoroalkyl, (C3-6) cycloalkyl, or (C1-4) alkyl, wherein the (C1-4) alkyl is unsubstituted or substituted with hydroxy, methoxy, ethoxy, OCH2CH2OH, -CN, imidazolidin-2-one, phenyl, or tetrazole wherein tetrazole is unsubstituted or substituted with (C1-4) alkyl; R2 is H, halogen, (C1-6) fluoroalkyl, (C3-6) cycloalkyl, OR6, SR6, NO2, CN, COR6, C(O)OR6, C(OH)R6, CONR7R8, phenyl or (C1-6) alkyl, wherein the (C1-6) alkyl is unsubstituted or substituted with a hydroxy; R3 is hydrogen, (C 1-6)fluoroalkyl , (C3-6) cycloalkyl, (C2-6) alkenyl, phenyl, monocyclic heteroaromatic, bicyclic heteroaromatic, or (C1-4)alkyl wherein (C1-4) alkyl is unsubstituted or substituted with a phenyl; R4 and R5 are independently selected from hydrogen, halogen, (C1-6) alkyl, (C1-6) fluoroalkyl, OR9, SR9, NO2, CN, or COR9; R6 is hydrogen, (C1-6) fluoroalkyl, or (C1-6) alkyl; R7 and R8 are independently hydrogen, or (C1-6) alkyl; R9 is hydrogen, (C1-6) fluoroalkyl, (C1-6) alkyl; Alk is (C1-4) alkylene unsubstituted or substituted with a hydroxy; Y is oxygen, sulfur, SO2, or a bond; X is CH2, C=O, S, O, or SO2; Z is hydrogen, halogen, (C1-6) alkyl, (C1-6)fluoroalkyl, -OH, (C1-6) alkoxy, (C1-6) fluoroalkoxy, (C1-6) alkylthio, (C1-6) acyl, (C1-4)alkylsulfonyl, -OCF3, -NO2, - CN, carboxamido which may be substituted on the nitrogen by one or two (C1-4) alkyl groups, and -NH2 in which one of the hydrogens may be replaced by a (C1-4) alkyl group and the other hydrogen may be replaced by either a (C1-4) alkyl group, a (C1-6) acyl group, or a (C1-4) alkylsulfonyl group; the phenyl of R1, R2 or R3 is independently unsubstituted or substituted with one to three substituents independently selected from Z; the monocyclic heteroaromatic of R3 is unsubstituted or substituted with one to three substituents independently selected from Z; the bicyclic heteroaromatic of R3 is unsubstituted or substituted with one to three substituents independently selected from Z; and salts, solvates, and crystal forms thereof. Also described are the use of the compounds of formula (I) as antagonists of the dopamine D2 receptor and as agents for the treatment of psychosis and bipolar disorders, and pharmaceutical formulations of the compounds of formula (I).
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Page/Page column 75

(2010/02/11)

PROCESS FOR PRODUCING DIBENZOTHIAZEPINE DERIVATIVES
A process for preparing a dibenzothiazepine derivative such as dibenzo[b,f] [1,4]thiazepin-11-one employable as a starting material for the preparation of 11-[4-(2-(2-hydroxyethoxy)ethyl)]-1-piperadinyldiberizothiazepine derivative which is known to be effective as an antipsychotic pharmaceutical, has the steps of reacting a nitrobenzene derivative with a thiosalicylic acid derivative, reducing the obtained 2-nitro-2'-carboxy-diphenylsulfide derivative, and subjecting the obtained 2-amino-2'-carboxy-diphenylsulfide derivative to dehydration-condensation reaction.
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(2008/06/13)

Antiviral dibenzothiazepinone derivatives
Compounds of formula (I) wherein n is 0, 1 or 2; and R1 and R2, which may be the same or different, each represent one or more ring substituent(s) selected from: hydrogen, hydroxy, halogen, cyano, nitro, C1-6 alkyl, C3-6 cycloalkyl or C1-6 alkoxy (where the alkyl or cycloalkyl moiety may be optionally substituted by one or more substituents selected from halogen atoms and hydroxyl groups); --NR4 R5 where R4 and R5, which may be the same or different, each represent hydrogen or C1-6 alkyl; --S(O)m R6, where m is 0, 1, 2 or 3 and R6 represents hydrogen, C1-6 alkyl or C3-6 cycloakyl; --SO2 NR4 R5 where R4 et R5 are each as defined above; phenyl, phenylC1-3 alkoxy or phenylC1-3 alkyl where the phenyl group may be optionally substituted by one or more substituents independently selected from C1-6 alkyl, C1-6 alkoxy, hydroxy, nitro, halogen and amino; and --CO2 H or --COR7 where R7 is C1-6 alkyl or C3-6 cycloalkyl; R3 represents hydrogen or C1-4 alkyl; and esters, salts and other physiologically functional derivatives thereof; show activity as antiviral agents, for example against HIV. Certain of the compounds are novel.
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(2008/06/13)

Dibenzothiazepinthione as antiviral agents
Compounds of formula (I) wherein n is 0, 1 or 2; and R1 and R2, which may be the same or different, each represent one or more ring substituent(s) selected from: hydroxy, halogen, cyano, nitro, C1-6 alkyl, C3-6 cycloalkyl or C1-6 alkoxy (where the alkyl or cycloalkyl moiety may be optionally substituted by one or more substituents selected from halogen atoms and hydroxyl groups); --NR4 R5 where R4 and R5 which may be the same or different, each represent hydrogen or C1-6 are each as defined above; phenyl, phenyl C1-3 alkoxy or phenyl C1-3 alkyl where the phenyl group may be optionally substituted by one or more substituents independently selected from C1-6 alkyl, C1-6 alkoxy, hydroxy, nitro, halogen and amino; and --CO2 H or --COR7 where R7 is C1-6 alkyl or C3-6 cycloalkyl; R3 is hydrogen or C1-4 alkyl: and esters, salts and other physiologically functional derivatives thereof, show activity as antiviral agents, for example against HIV. The majority of the compounds are novel.
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(2008/06/13)

Dibenz[b,f][1,4]oxazepin(and thiazepin)-11(10H)-ones and-thiones and their use in the prevention or treatment of HIV infection
Disclosed is the use of dibenz[b,f][1,4]oxazepin (or thiazepin)-11(10H)-ones and -thiones in the prevention and treatment of AIDS, ARC and related disorders associated with HIV infection.
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(2008/06/13)

MUSCARINIC RECEPTOR LIGANDS
Described herein are D4 receptor-selective compounds of the general formula I: STR1 wherein: A and B are independently selected, optionally substituted, saturated or unsaturated 5-or 6-membered, homo-or heterocyclic rings;X 1 is selected from CH 2, O, NH, S, C=O, CH--OH, CH--NEt 2, C=CHCl, C=CHCN, N--C. sub.1-4 alkyl, N-acetyl, SO 2 and SO;X 2--is selected from N=, CH 2--, CH=, C(O)--, O--, and S--; n is 1 or 2; andZ is selected from C 1-6 alkyl optionally substituted with a substituent selected from OH, halo, C. sub.1-4 alkyl and C 1-4 alkoxy;and acid addition salts, solvates and hydrates thereof. Their use as ligands for dopamine receptor identification and in a drug screening program, and as pharmaceuticals to treat indications in which the M1/M2 receptor is implicated, such as schizophrenia, is also described.
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(2008/06/13)

NOVEL REACTIONS OF SPIROSULFURANE PRECURSOR SULFIDES AND SULFOXIDES
The SIV spirosulfurane 19 and the lactam-sulfoxides 21, 22 and 23 with seven-, eight- and nine-membered rings have been prepared by oxidation and dehydration of trifluoroacetylaminoarylcarboxyphenyl sulfides and sulfoxides, respectively.A mechanism is proposed for the formations of lactam-sulfoxides.The preparation of the starting sulfides and sulfoxides is also described. Key words: Diaryl sulfides; diaryl sulfoxides; spirosulfurane; lactams; carboxyl activation; lactam-sulfoxide formation.
Kuti, M.,Rabai, J.,Kapovits, I.
p. 119 - 128
(2007/10/02)

NOVEL DIBENZOTHIAZEPINE ANTIPSYCHOTIC
11-[4-[2-(2-Hydroxyethoxy)ethyl]-1-piperazinyl]dibenzo[b,f][1, 4 ] thiazepine is disclosed as a neuroleptic with a much reduced incidence of side effects such as acute dystonia and dyskinesia and tardive diskinesia.
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(2008/06/13)

10,11-dihydro-dibenzo-[b,f][1,4]-thiazepin derivatives
Compounds of the Formula I: STR1 are inhibitors of the mammalian 5-lipoxygenase enzyme system of the arachidonic acid cascade. As such, these compounds are useful therapeutic agents for treating allergic conditions, asthma, cardiovascular disorders and inflammation and are useful as cytoprotective agents.
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(2008/06/13)

Process for the preparation of a thiazepine compound
11-(4-[2-(2-Hydroxyethoxy)ethyl]-piperazinyl)-dibenzo[b,f][1,4]thiazepine and the salts thereof possess antiandropaninergic activity, especially antipyschotic activity, and are prepared by reacting 11-piperazinyldibenzo[b,f][1,4]thiazepine with a compound of the formula:-, X-CH2-CH2-O-CH2-CH2OH, (wherein X represent an atom or group removable as an anion and, where appropriate further reaction of the product obtained to yield the free base or salt as desired.
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(2008/06/13)

Photochemical Ring-expansion Reaction of 1,2-Benzisothiazolinones
The photochemical reaction of a series of 2-aryl-1,2-benzisothiazol-3(2H)-ones (1) under deaerated conditions was found to give dibenzothiazepin-11(10H)-ones (2).A mechanism through a biradical species is proposed for the photoreaction.When the photolysis of 1 was carried out in the presence of oxygen, 2-aryl-1,2-benzisothiazol-3(2H)-one-1-oxides (11) were formed together with compounds 2.
Kamigata, Nobumasa,Hashimoto, Satoshi,Kobayashi, Michio,Nakanishi, Hiroshi
p. 3131 - 3136
(2007/10/02)

3-(4-Methylpiperazino)dibenzo[b,f]-1,2,4-triazolo[4,3-d]-1,4-4-thiazepine and its 6-chloro and 12-chloro derivatives; synthesis and pharmacology
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Polivka,Holubek,Svatek,et al.
p. 1465 - 1476
(2007/10/02)

Synthesis of 11-Oxo and 11,11-Diphenyl Derivatives of Dibenzothiazepines, Dibenzooxazepines and Dibenzodiazepines
11-Oxo (IIa-c) and 11,11-diphenyl (IVa-c) derivatives of dibenzothiazepine, dibenzooxazepine and dibenzodiazepine have been prepared by treating the lithiated intermediates with carbon dioxide and benzophenone respectively.
Shete, N. R.
p. 581 - 582
(2007/10/02)