- Benzisothiazole hypoxia-inducible factor 2 agonist compound or pharmaceutically acceptable salt, preparation method and application thereof
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The invention discloses a benzisothiazole hypoxia-inducible factor 2 agonist compound or a pharmaceutically acceptable salt thereof, the compound can stimulate the transcriptional activity of a hypoxia-inducible factor 2 and enhance the generation and secretion of erythropoietin so as to promote the generation of erythrocytes; the prepared benzisothiazole hypoxia-inducible factor 2 agonist compound or the pharmaceutically acceptable salt thereof can be combined with a prolyl hydroxylase inhibitor to play a synergistic role in improving the transcriptional activity of HIF-2, and can be used for treating hypoxia-inducible factor 2 related diseases, such as ischemic diseases and the like.
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- 3 - Aminobenzo [d] isothiazole. Derivative and synthesis method thereof
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The invention mainly relates to 3-aminobenzo[d]isothiazole and derivatives thereof and a synthetic method thereof. Benzamidine compounds and elemental sulfur are converted into 3-aminobenzo[d]isothiazole and the derivatives thereof only under the action of an alkali and in an air atmosphere without use of a catalyst during synthesis. The problems that a conventional synthetic method of a functionalized 3-aminobenzo[d]isothiazole compound has complex synthetic steps, requires a multistep synthesis process to complete, and also requires use of metal catalysts or peroxides, as well as has low yield or harsh reaction conditions are overcome. The synthetic method has the characteristics of simple reaction system, mild reaction conditions, less reaction equipment, simple experimental operation,wide sources of used materials, high yield, easy expanding of users and application, high utilization value of products, expectable prospects of commercialization of the market and the like.
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Paragraph 0069; 0084-0090; 0093
(2021/05/08)
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- Efficient synthesis of 1,2-benzisothiazoles from: O -haloarylamidines and elemental sulfur via N-S/C-S bond formation under transition-metal-free conditions
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An efficient method for the synthesis of 1,2-benzisothiazoles from amidines and elemental sulfur via N-S/C-S bond formation under transition-metal-free conditions is described. This reaction is performed smoothly under simple conditions to give the corresponding products in good to high yields with good functional group tolerance.
- Xie, Hao,Li, Guozheng,Zhang, Feng,Xiao, Fuhong,Deng, Guo-Jun
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supporting information
p. 827 - 831
(2018/03/02)
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- 3-Amino-1H-pyrazolopyrimidines and 3-Aminoisothiazolopyrimidines as Precursors of Tricyclic Heteroaromatic Systems Containing a Bridgehead Nitrogen Atom.
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3-Amino-4-methyl-6-phenyl-1H-pyrazolopyrimidine (3a) and 3-amino-4-methyl-6-phenylisothiazolopyrimidine (9a) have been prepared.The former reacts with bromoacetone or 3-bromopentane-2,4-dione, to give tricyclic systems (1a) or (13) containing an extra pyrazole or pyrimidine ring, respectively; in each case the newly formed ring contains a bridgehead nitrogen atom, derived from N-2 of the starting material.With the same reagents, the latter undergoes an interesting ring-opening reaction, for which possible mechanisms are proposed.In contrast, 3-amino-1,2-benzisothiazole does not undergo ring fission under similar conditions, but gives rise to tricyclic compounds containing a bridgehead nitrogen atom.
- Golec, Julian M. C.,Scrowston, Richard M.
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p. 326 - 345
(2007/10/02)
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