- Quinazolinone Compound and Application Thereof
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The present invention relates to a series of quinazolinone compounds and applications thereof as PI3Kα inhibitors. In particular, the present invention relates to a compound shown in formula (I) and a tautomer or pharmaceutically acceptable salt thereof.
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Paragraph 0804-0806
(2020/11/27)
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- Preparation method of intermediate for preparing tianeptine sodium
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The invention discloses a preparation method of an intermediate compound for preparing tianeptine sodium. The intermediate compound is shown as a formula. According to the synthesis method, p-chlorotoluene is used as a starting raw material to react with chlorosulfonic acid to obtain sulfonyl chloride, the sulfonyl chloride undergoes an amidation reaction with N-methylaniline under alkaline conditions to obtain sulfonamide, an aqueous solution of the sulfonamide and air are continuously pumped into a fixed bed reactor loaded with an immobilized catalyst according to a certain ration for oxidation to obtain carboxylic acid, and then the carboxylic acid is subjected to cyclization under catalysis of a solid acid to obtain the target compound. The method has simple and few steps, the cost ofthe raw materials is low, the fixed bed reactor and the solid acid catalyst are utilized, the catalyst can be repeatedly recycled to reduce the discharge of the three wastes, the production process isenvironmentally friendly, and the method is more suitable for industrial production.
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Paragraph 0020-0022; 0029-0031
(2019/09/05)
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- Some new 1,2-benzothiazine derivatives with analgesic and anti-inflammatory activities
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Twenty-three new 7-halo-4-hydroxy-2H(or alkyl)-N-(3-aralkyl-2-thio-l-hydantoinyl)-2H- 1,2-benzothiazine-3-carboxamide 1,1-dioxide derivatives were synthesized through the condensation of 7-halo-4-hydroxy-2H(or alkyl)-1,2-benzothiazine-3-carboxylic acid methyl ester 1,1-dioxides with 1-amino-2-thio-3-aralkyl-imidazolidine-4-one. The analgesic and anti-inflammatory activities of the synthesized compounds were investigated by acetic acid-induced writhing syndrome and carrageenan rat paw edema tests. In analgesic activities most compounds exhibited higher activities than acetylsalicylic acid, but in antiinflammatory activities most compounds except compounds 24, 36, 39 showed lower activities than indometacin.
- Kwon, Soon-Kyoung,Park, Myung-Sook
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p. 966 - 971
(2007/10/03)
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- Herbicidal sulfonamides
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4-Chloro-2-[[(4-methoxy-6-methyl-1,3,5-triazin-2-yl)aminocarbonyl]aminosulfonyl]benzoic acid (1-methylethyl) ester has unexpectedly been discovered to be an outstanding agricultural chemical. The compound is a highly active preemergent and/or postemergent herbicide. The invention includes the compound, compositions containing the compound, and its method-of-use as an agricultural chemical.
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