54201-83-1Relevant articles and documents
Environmentally-friendly synthesis method of ulipristal acetate intermediate and ulipristal acetate
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, (2020/07/14)
The invention provides a method for environmentally-friendly synthesis of an ulipristal acetate intermediate and ulipristal acetate. According to the invention, a compound 2 is used as a starting rawmaterial, and reacts with acetylene in a solvent to form an alkynyl alcohol compound intermediate 3, a hydration reaction is performed with water under the catalysis of an ionic liquid and CO2 to obtain an intermediate 4, the intermediate 4 is subjected to carbonyl protection to obtain an intermediate 5, and the intermediate 5 is subjected to double bond epoxidation, a Grignard reaction, decarbonylation protection and acetylation to obtain the high-purity ulipristal acetate. The method is environment-friendly, convenient in steps, mild in conditions, low in cost, easy to amplify and suitable for industrial production, and the solvent can be recycled.
Cyclic utilization method of sterides epoxy isomer
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, (2018/06/04)
The invention provides a cyclic utilization method of sterides epoxy isomer. Biphenyl organic solvent is reacted with active metal lithium, sodium, and potassium, and others, and reduced to be conjugated double bond; under the alkali environment, the ketal protection radical group is not influenced, and 17- hydroxyl is also not influenced, thus the position of double bond is not changed and doublebonds are directly transformed to be raw material of the last step, and the raw materials are recycled. The method adopts one-step reduction, and solves the existing common technique of opening loopof epoxy bond firstly and then dewatering to be double bonds, and avoids that the ketal protection radical can be damaged by directly reducing epoxy bond to be double bonds by metal in the alkali environment; the epoxy isomer beta and a part of alpha isomer are directly reduced to be the raw material containing conjugated double bond in last step, thus a simple cycle is realized.
Ulipristal acetate impurities and preparation and detection method thereof
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Paragraph 0111, (2017/03/08)
The invention provides ulipristal acetate impurity compounds and a preparation method thereof, and particularly provides a novel compound impurity F (a compound F) and a novel compound impurity K (a compound K). The invention further provides a detection method of the impurities and application of the impurities on quality analysis of an ulipristal acetate bulk drug and a preparation thereof.