The patent 162542, granted to the Institute of Pharmaceutical Industry in Warsaw (the owner), presents new pharmacologically active analogues of vitamin D3.
The vitamin D3 compounds (vitamin D3 analogues) affect calcium metabolism in human organism.
They are antileukemic and can be used in a therapy of leukemia (leukaemia).
They may be used in dermatology.
The starting compound is methyl ester of (5Z,7E)-(1S,3R)-1-hydroxy-3-acetoxy-9,10-seco-5,7,10(19)-cholatrien-24-oic acid.
It is treated with t-butyldimethylsilyl chloride. Then after reduction and Swern oxidation an aldehyde is obtained.
This aldehyde reacts with the second compound, main part of which is the side chain of the target molecule.
This second compound is a sulfon, obtained from 3-bromopropionic acid in a series of reactions.
A hydroxyl group in this sulfon is protected as triethylsilyl derivative.
The patented process is cheap and effective, and does not require any dear chemicals, and the vitamin D derivatives may be used as potent antileukemic agents and in dermatology against skin deseases.
