- A berberine of the preparation method of the key intermediate
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The invention discloses a preparation method of a key intermediate of berberine. The method comprises the following steps: enabling pepper benzyl chloride to react with malonic acid diester under the action of organic alkali, so as to obtain pepper diester benzylmalonate; carrying out decarboxylation on the pepper diester benzylmalonate under the catalysis of strong alkali; enabling pepper propionic acid to react with phosphorus pentachloride in an organic solvent, so as to obtain pepper propionyl chloride; enabling pepper propionyl chloride to react with ammonia gas or ammonia water in the organic solvent, so as to obtain pepper propanamide; and carrying out Hoffman rearrangement reaction on propanamide under the common action of sodium hypochlorite or chlorine gas or sodium hydroxide, so as to obtain the pepper ethylamine. According to the method disclosed by the invention, raw materials are available, the operation is simple, the reaction condition is mild, and industrial production can be achieved easily.
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Paragraph 0023-0024; 0027-0028
(2018/05/16)
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- Sulfonic acid ester derivatives, method for production thereof and use thereof
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Novel and useful optical active 2-aralkyl-3-sulfonyloxy-1-propanol and 2-aralkyl-3-sulfonyloxypropionic acid are provided by using an optical active 2-aralkyl-3-acyloxy-1-propanol as a starting material. Furthermore, an optical active 2-aralkyl-3-thiopropionic acid, which is an important intermediate of enkephalinase inhibitor, is provided. According to the present invention, industrially useful optical active sulfonic acid ester derivatives can be provided.
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Page column 11
(2010/02/05)
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- Process for the synthesis of α-substituted acrylic acids and their application
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Process for the synthesis of a-substituted acrylic acids and their application. Process for the synthesis of a-substituted acrylic acids of general formula (I) and their application to the synthesis of N- (mercaptoacyl) aminoacid derivatives of formula (II). STR1
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