Novel side chain of 25-hydroxyitamin D2 series medicines and preparation method thereof

Abstract

The invention relates to a preparation of organic compounds, in particular to a preparation method of a common side chain of a series of 25-hydroxyitamin D2 medicines. The structure of the compounds is represented in the formula 1. The compounds have wide application and are more stable than the traditional compounds with the same application, so that the compounds are convenient to storage and use. The method for synthesizing the target compounds (1) has high yield, short synthesis route and easily purified products.

Description

technical field The present invention relates to a method for preparing an organic compound, specifically a method for preparing a series of common side chains of 25-hydroxyvitamin D2 drugs, the structure of which is shown in Formula 1 below. Formula 1 Among them, R is a hydrogen atom or -SiR 3 R 4 R 5 or -R 3 or -R 6 OR 4 or -C(=O)R 3 , where R 1 , R 2 , R 3 , R 4 , R 5 , R 6 are hydrocarbyl or hydrocarbyloxy or amino or hydrocarbyl-substituted amino, and they may be the same or different. Background technique Formula 2 Formula 3 A series of 25-hydroxyvitamin D2 drugs shown in formula 2 have a common side chain, and these drugs can be synthesized from compound 1 through the process shown in formula 3. These drugs include 25-hydroxyvitamin D2, 1a, 25-dihydroxyvitamin D2, paricalcitol, and others. These drugs are regulators of calcium and phosphorus homeostasis in animals and humans 1，2 . Recent studies have also identified their activity in cell ...

AI Technical Summary

Problems solved by technology

Compound 5 not only has a low yield when it is used for drug synthesis, but also the synthesis and purification of compound 5 itself is difficult, and its synthesis process also causes some limitations for the protective group R functional group

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