953789-37-2Relevant articles and documents
Method for preparing lorcaserin
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Paragraph 0025-0028, (2020/08/22)
The invention discloses a method for preparing lorcaserin. Specifically, the method comprises the steps: taking p-chlorophenylacetonitrile as an initial raw material, preparing p-chlorophenylethylamine through reduction; carrying out a reaction with p-toluenesulfonyl chloride to form an amino occupying intermediate; enabling the intermediate to carry out a reaction with monochloroacetone under analkaline condition to form N-(2-(4-chlorphenyl)ethyl)-4-methyl-N-(2-propionyl)benzenesulfonamide, and then carrying out reduction, chlorination, p-toluenesulfonyl removal and intramolecular Friedel-Crafts alkylation to synthesize 8-chloro-1-methyl-2,3,4,5-tetrahydro-1H-3-benzoazepine, carrying out L-(+)-tartaric acid resolution and alkalization on azepine to remove tartaric acid, and acting with hydrogen chloride diethyl ether to salify to prepare lorcaserin. The method has the characteristics of simple synthesis method, good reaction selectivity, high product purity, environmental protectionand low preparation cost.
Preparation method of key intermediate I of lorcaserin
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Paragraph 0058; 0060-0061, (2018/09/26)
The invention discloses a preparation method of a key intermediate I of lorcaserin. The preparation method comprises the steps as follows: (1) in an organic solvent A, 2,4'-dichloroacetophenone is subjected to a condensation reaction with isopropanolamine under catalysis of alkali, and 1-(4-chlorophenyl)-2-((2-hydroxypropyl)amino)ethane-1-one is obtained; (2) the 1-(4-chlorophenyl)-2-((2-hydroxypropyl)amino)ethane-1-one obtained in the step (1) is subjected to catalytic reduction with sodium borohydride and acid in a solvent B, and the key intermediate I of lorcaserin is obtained. The preparation method can synthesize the key intermediate I of lorcaserin from cheap and easily available raw materials under mild reaction conditions, has the advantages of being simple to operate, low in costand high in yield, and is energy-saving, environmentally friendly and suitable for mass production.
1 - (phenethyl-amino) propane-2-ol compound or its salt for the preparation of
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Paragraph 0076; 0079-0080, (2016/11/24)
The invention relates to a preparation method of 1-(phenethylamino) propane-2-alcoholic compounds or salts thereof, shown in a formula II. The preparation method comprises the following step: reacting a compound shown in a formula I with epoxy propane to generate a compound shown in the formula II. According to the preparation method provided by the invention, cheap and accessible raw materials are adopted to prepare a target compound through a one-step reaction, so that the preparation method is low in cost, simple and convenient to operate, high in yield, environmental-friendly and suitable for industrial production. The invention also relates to a preparation method of lorcaserin or salts thereof. The lorcaserin is prepared from the high-purity 1-((4-chlorophenethyl) amino) propane-2-alcohol or the salts thereof, thereby being beneficial to improvement of the quality and stability of the product.