- Facile synthesis of bioactive 4H-[1,4]-benzothiazines under solvent free conditions
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An efficient method for synthesis of 4H-[1,4]-benzothiazines under solvent free conditions has been developed. The oxidative condensation of 2-aminobenzenethiols with β-diketones/β-ketoesters in presence of catalytic amount of hydrazine hydrate yields the 4H-[1,4]-benzothiazines. The reaction is accelerated by microwave irradiation under solvent free conditions in presence of an energy transfer agent DMF to get the product in high yield. The 2-aminobenzenethiazole required for the synthesis of 4H-[1,4]-benzothiazines are also obtained by a new method instead of presently used time consuming and low yielding method. The structure of the synthesized compounds has been characterized by IR, NMR, mass spectral studies and elemental analysis.
- Kalwania,Chomal,Choudhary, Savita
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p. 5133 - 5136
(2012/06/18)
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- Syntheses and evaluation of fluorinated benzothiazole anilines as potential tracers for β-amyloid plaques in Alzheimer's disease
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[11C]2-(4′-(Methylamino)phenyl)-6-hydroxybenzothiazole ([11C]PIB) is a most potential PET tracer for detecting the β-amyloid plaques in Alzheimer's disease. Here the syntheses of three fluorinated PIB, namely 2-(4′-(methylamino)phenyl)-6-fluoroethoxybenzothiazole (O-FEt-PIB), 2-(4′-(methylamino)phenyl)-6-fluoro-benzothiazole (F-N-Me) and 2-(4′-(dimethylamino)phenyl)-6-fluorobenzo-thiazole (F-N,N-Me), and the radiosynthesis of one corresponding 18F-labeled PIB compound, [18F]O-FEt-PIB, as well as their in vitro/in vivo biological characters were reported. The structures of the products were confirmed by IR, 1H NMR, EI/ESI-MS, elemental analysis and HRMS techniques. The radiolabeled product was characterized by radio-TLC and radio-HPLC and purified by semi-preparative radio-HPLC. The suitable biological characters showed these tracers were potential to be developed as probes for detecting β-amyloid plaques in Alzheimer's disease.
- Zheng, Ming-Qiang,Yin, Duan-Zhi,Qiao, Jin-Ping,Zhang, Lan,Wang, Yong-Xian
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p. 210 - 216
(2008/09/17)
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- Microwave-induced one pot synthesis and biological screening of 8-substituted-2,5-dihydro-1,5-benzothiazepin-2-spiro-3'-3'H-indol-2'-(1'H)-ones
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A convenient method for the synthesis of 8-substituted-2,5-dihydro-1,5-benzothiazepin-2-spiro-3'-3'H-indol-2'-(1'H)-ones, by one pot procedure under microwave irradiation, using ethylene glycol as energy transfer medium, is described. Results are compared
- Dandia, Anshu,Upreti, Mani,Rani, Babita,Pant, Umesh C.
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p. 3348 - 3355
(2007/10/03)
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- Synthesis of some new 1,4-benzothiazines and their anti psychotic activity
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1,4-Benzothiazines (1-28) have been synthesized by treating substituted aminothiophenols with various substituted β-diketones in the presence of piperidine in THF solution.
- Chaudhari,Shinde,Shingare
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p. 1250 - 1256
(2007/10/03)
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- PYRIMIDO-BENZOTHIAZINES
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This invention relates to novel pyrimido-benzothiazine derivative compounds. The compounds of the present invention inhibit the action of the lipoxygenase enzyme and are useful in the treatment or alleviation of inflammatory diseases, allergy and cardiovascular diseases in mammals. this invention also relates to pharmaceutical compositions comprising such compounds.
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- Synthesis and antihypertensive activity of 3-acetoxy-2,3-dihydro-5-[2-(dimethylamino)ethyl]-2-(4-methoxyphenyl)-1 ,5-benzothiazepin-4(5H)-one (diltiazem) derivatives having substituents at the 8 position
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In order to improve the potency and duration of biological actions of diltiazem, a number of 1,5-benzothiazepine derivatives having the substituents at the 8 position were prepared and evaluated for their antihypertensive activity in spontaneously hyperte
- Yanagisawa,Fujimoto,Shimoji,Kanazaki,Mizutari,Nishino,Shiga,Koike
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p. 2055 - 2061
(2007/10/02)
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- Syntheses of 1,5-Benzothiazepines: Part III - Syntheses of 4-(p-Chlorophenyl)-2-(p-methoxyphenyl)-8-substituted-2,3-dihydro-1,5-benzothiazepines
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4-Methoxy-4'-chlorobenzalacetophenone (IV) on reaction with 5-substituted 2-aminothiophenols (IIIa-f) in toluene gives 4-(p-chlorophenyl)-2-(p-methoxyphenyl)-8-substituted-2,3-dihydro-1,5-benzothiazepines (Va-f).Their structures have been established by IR, PMR and mass spectral data.
- Pant, Umesh C.,Gaur, B. S.,Chugh, Manju
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p. 189 - 190
(2007/10/02)
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- A CONVENIENT AND SINGLE STEP SYNTHESIS OF SUBSTITUTED 4H-BENZOTHIAZINES.
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A simple one step synthesis is reported for substituted 4H-benzothiazines involving the condensation of 5-(chloro, bromo, methyl, methoxy, ethoxy)-, 4-methyl- and 3-(chloro and methoxy)-2-aminobenzenethiols with acetylacetone/ethyl acetoacetate/dibenzoylmethane in DMSO.
- Gupta, R. R.,Ojha, K. G.,Kalwania, G. S.,Kumar, M.
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p. 1145 - 1149
(2007/10/02)
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