- Method for preparing 2-amino-4-aminomethyl methyl benzoate and hydrochloride thereof
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The invention relates to the field of organic synthesis, and discloses a method for preparing 2-amino-4-aminomethyl methyl benzoate and hydrochloride thereof. The method comprises the following steps:1) sequentially contacting dimethyl terephthalate with a nitration reagent and acetic acid to obtain 3-nitro-4-methoxycarbonyl benzoic acid; (2) converting the 3-nitro-4-methoxycarbonyl benzoic acidinto 2-nitro-4-methoxycarbonyl benzoyl chloride, and enabling the 2-nitro-4-methoxycarbonyl benzoyl chloride to be in contact with ammonia gas so as to obtain methyl 2-nitro-4-formylaminobenzoate; 3)performing dehydration reaction on the 2-nitro-4-formylaminobenzoic acid methyl ester to obtain 2-nitro-4-cyanobenzoic acid methyl ester, and 4) performing reduction reaction on the 2-nitro-4-cyanobenzoic acid methyl ester to obtain 2-amino-4-aminomethyl benzoate. The preparation method has the advantages of high yield, high purity and environmental protection.
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Paragraph 0051; 0054-0055; 0060; 0063-0064; 0073-0076
(2020/09/08)
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- 2-amino-4-methanesulfonamide preparation of methyl benzoic acid methyl ester
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The invention relates to a method for preparing 2-amino-4-methanesulfonamide methylbenzoate. According to the method, dimethyl terephthalate serves as a raw material, and then 2-amino-4-methanesulfonamide methylbenzoate is prepared through nitrification, ammonolysis, dehydration, hydrogenation reduction and sulfonylation. The method has the advantages that the raw material is easy to obtain, the reaction conditions are mild, the yield is high, the byproducts are few, the pollution is little, and the like; the difficult problems in the existing mesosulfuron-methyl preparation processes that the raw material is expensive, the conditions are harsh, the pollution is serious, and the like are solved effectively.
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Paragraph 0029; 0032; 0033
(2017/02/09)
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- FUROISOQUINOLINE DERIVATIVE AND USE THEREOF
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The present invention provides a compound represented by the formula ???wherein A represents (1) a bond, (2) a group represented by the formula -CRa=CRb- (Ra and Rb each represent a hydrogen atom or C1-6 alkyl) and the like; R1 represents (1) cyano or (2) an optionally esterified or amidated carboxyl group; R2 represents(1) a hydrogen atom, (2) an optionally substituted hydroxy group,(3) an optionally substituted amino group and the like; R3 and R4 each represent a hydrogen atom and the like; R5 represents a hydrogen atom and the like; R6 represents an optionally substituted hydroxy group and the like; R7and R8 each represent an optionally substituted hydrocarbon group and the like; R9 and R10 each represent (1) a hydrogen atom and the like; Y represents an optionally substituted methylene group; and n represents 0 or 1, or a salt thereof, which has an excellent phosphodiesterase IV inhibiting action.
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Page/Page column 67
(2010/02/11)
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