Method for preparing ergocalciferol double-projection product

Abstract

The invention discloses an improved method for preparing an ergocalciferol double-projection product, which is characterized by comprising the following steps: a) adding ergocalciferol in liquid sulfur dioxide, and respectively reacting at minus 25-minus 10 DEG C, at room temperature and at 30-40 DEG C; b) directly adding tert-Butyldimethylsilyl chloride and imidazole to react; and c) adding alkane solvent, and recrystallizing to obtain a target product. The invention adopts a one-pot method to merge at two-step reaction into one-step reaction, thus lowering the solvent cost and reducing other energy consumption at the same time; and a recrystallization method instead of column chromatograph is adopted to obtain the target product so as to enable the method to be applicable to industrialized production in technology.

Description

technical field

[0001] The present invention relates to the production of vitamin D2 double protection product (9.10-ring-opened cholesteryl-5,7(E)10,19,22(E)-tetraene-3S-tert-butyldimethylsilyl ether sulfur dioxide adduct) Preparation. Background technique

[0002] Vitamin D in the classical sense refers to some sterol substances for the treatment and prevention of rickets, including vitamin D2 and calciferol, vitamin D3 and vitamin D1 (or vitamin D4). Vitamin D2 and vitamin D3 have an important impact on calcium and phosphorus metabolism and bone growth in children. They can promote calcium and phosphorus absorption in the intestine and normal bone calcification. They are the main drugs for the treatment of rickets, rickets and hypothyroidism clinically.

[0003] Although vitamin D2 and vitamin D3 have the same effect, they have different activity strengths. In comparison, the strength of vitamin D3 is greater than that of vitamin D2, and some active metabolites of vitami...

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