Synthesis method for everolimus

The invention provides a synthesis method for everolimus. The synthesis method comprises the following steps: 1, preparation of an everolimus silicon etherification product (a midbody A); 2, hydrolysis reaction: generating the reaction between the midbody A and inorganic acid or hydrofluoric acid or...

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Hauptverfasser: YANG GUOXIN, HUANG JIE, LI KUALIANG, YING JIAYIN, YU HUI, CHEN XIAQIN, XIE LIJUN, CHENG YUANRONG, JIN DONGWEI
Format: Patent
Sprache:eng
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Zusammenfassung:The invention provides a synthesis method for everolimus. The synthesis method comprises the following steps: 1, preparation of an everolimus silicon etherification product (a midbody A); 2, hydrolysis reaction: generating the reaction between the midbody A and inorganic acid or hydrofluoric acid organic alkali in an organic solvent to obtain everolimus, and finally obtaining the target product, everolimus. According to the synthesis method, in the first reaction step, DIPEA (diisopropylethylamine) is used as alkali, methylbenzene is used as a solvent, and a brand-new feeding method and a post-treatment method are adopted, so that the reaction time is greatly shortened; moreover, the purity and the yield of the everolimus silicon etherification midbody are greatly improved. Due to optimization and selection of the reaction conditions, particularly the feeding method and the post-treatment method are greatly and technically improved, so that the universality key problem in the product synthesis process is solved; by two steps, the total yield and the final product purity are greatly improved much more than those in the existing literature reports.