PROCESS AND INTERMEDIATES TO PREPARE THE SULPHONYL DERIVATIVES OF CHOLECALCIFEROL

摘要

Preparation of sulphonyl derivatives of cholecalciferol of Formula (I), wherein R₁ is protective group, preferably t-butyl(dimethyl)silyl, where R₂ is heterocyclic group, such as 2-thiazolyl, 2-benzothiazolyl, 1-phenyl-lH-tetrazo-5-yl, 2-pyridyl, 2-pyrimidynyl, 1-isochinolinyl, 1-methyl-2-imidazyl, 4-alkyl-1,2,4-triazo-3-yl, comprising the conversion of the hydroxyl derivative of cholecalciferol into the corresponding sulfide followed by its oxidation to the respective sulphone characterized by the use of hydroxyl derivative of cholecalciferol as a starting material, which triene system is protected as Diels-Alder adduct, and in particular as an adduct with sulfur dioxide of the formula 2a. Novel are derivatives of formula 3a and 4, isolated in the process provided in the invention.