- Synthetic process of prenestyene (by machine translation)
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The invention belongs to the technical field of drug synthesis, and particularly relates to a synthetic process. The method comprises the following steps: taking estradiol as a raw material, carrying out a halogenation reaction with halogenated reagent under catalysis of a solid acid catalyst, producing 3 - hydroxyl - 17 17 17, (-1) - triene, synthesizing 3 propoxy - 17 17 17 beta-methoxyestrostane 5, 10, 1 - (3 3 - 5) - 10 triene; solid acid catalyst being a sulfonated carbon-based solid acid catalyst or ZSM - 5 molecular sieve catalyst by Willililison synthesis reaction and reaction, finally reacting with -1 bromopropane with sodium methoxide methanol solution. To the invention, hydrobromic acid and sodium methoxide are used to replace dimethyl sulfate with high dangerousness, the reaction is free of inflammable gas generation, environmental pollution and potential safety hazards, and the product yield and quality, HPLC purity is higher higher higher, 99.8% and the method is suitable 0.05% for industrial production. (by machine translation)
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Paragraph 0036-0050
(2019/10/01)
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- Synthesis method of promestriene
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The invention relates to a synthesis method of compound promestriene. The compound is a derivative of estradiol, has characteristics of estrogen and has a significant effect of regulating and promoting normal development of female sexual organs and secondary sexual characteristics. Estradiol is used as a starting material, sodium hydroxide is adopted for base catalysis and subjected to a reactionwith n-bromopropane in an acetone solvent, and 3-propoxy-17beta-hydroxyestr-1,3,5(10)-triene is prepared; promestriene is prepared from sodium hydride as an alkaline catalyst and methyl iodide as a methylation reagent in a tetrahydrofuran solvent. The synthesis method has the advantages that reaction conditions are mild, toxicity of the solvents or reagents is low, post-treatment is convenient, the yield is high and synthesis cost is low, and the synthesis method is environmentally friendly.
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Paragraph 0022; 0026-0026
(2019/07/29)
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