- Preparation method of 3-methyl-2-aminobenzoic acid
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The invention discloses a preparation method of 3-methyl-2-aminobenzoic acid. The preparation method comprises the steps that 2-chloro-m-xylene is added into an acetic acid solvent for stirring, sodium acetate is added as a catalyst, the temperature is raised to 80-100 DEG C by heating, hydrogen peroxide is dropped for a reaction, after the reaction, 3-methyl-2-chlorobenzoic acid is obtained through rectification under vacuum; the 3-methyl-2-chlorobenzoic acid is added into a DMSO solvent, and catalysts of copper chloride and sodium carbonate are added and heated to 120-140 DEG C, and then ammonia is introduced and heated to 150-160 DEG C for a heat preservation of 3-6 hours, and the 3-methyl-2-aminobenzoic acid is obtained. According to the preparation method, a new design idea is provided for the synthesis of the 3-methyl-2-aminobenzoic acid, the preparation method is simple, operation is easy, the cost is low, and the preparation method is environmentally friendly.
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Paragraph 0015-0017
(2019/11/12)
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- 2 - Chloro -3 - methyl benzoic acid and intermediate preparation method (by machine translation)
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The invention discloses a 2 - chloro - 3 - methyl benzoic acid and intermediate preparation method. A 2 - chloro - 3 - methyl benzoic acid and intermediate preparation method, comprising the following steps, in the oxygen pressure is 0.1 mpa - 0.8 mpa under the condition of, under the action of the catalyst and promoter, the 2, 6 - dimethyl chlorobenzene to carry out oxidation reaction, can be; wherein said 2, 6 - dimethyl chlorobenzene and the oxygen molar amount ratio of 1: 1.8 - 1: 2.2. The 2 - chloro - 3 - methyl benzoic acid, in order to industrially easily available raw materials for the reaction, after treatment is simple, high yield, purity is good, small pollution to the environment, is more suitable for industrial. (by machine translation)
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Paragraph 0103; 0104
(2018/10/11)
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- AMINO ACID DERIVATIVES AND THEIR USE AS THROMBIN INHIBITORS
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There is provided compounds of formula I, wherein R 1, R 2, R 3, R x, Y, n and B have meanings given in the description which are useful as competitive inhibitors of trypsin-like proteases, such as thrombin, and in particular in the treatment of conditions where inhibition of thrombin is required as in thrombosis or as anticoagulants.
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- 3-aroylbenzylpyridazinone derivatives
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Compounds of formula I: STR1 where: R10 is a group represented by formula (A), (B), or (C): STR2 and the other substituents are as defined in the specification; and their pharmaceutically acceptable salts are inhibitors of prostaglandin G/H synthase and are anti-inflammatory and analgesic agents.
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- 6-Benzyl-2H-pyridazin-3-one derivatives,their preparation and their use as inhibitors of prostaglandin G/H synthase I and II (COX I and COX II)
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Compounds of formula I: where: the dashed line denotes an optional bond; R1is H, halo, alkyl, alkyloxy, amino, alkylamino, dialkylamino, or acylamino; R3and R4are independently H, halo, alkyl, alkyloxy, or hydroxy; R5
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