Process and Intermediates for the Preparation of Sulfonyl Derivatives of Cholecalciferol

Preparation of sulfonyl derivatives of cholecalciferol of Formula 1, wherein R1 is a protective group, preferably a t-butyl(dimethyl)silyl, and R2 is a heterocyclic group, such as a 2-thiazolyl, a 2-benzothiazolyl, a 1-phenyl-1H-tetrazo-5-yl, a 2-pyridyl, a 2-pyrimidynyl, a 1-isochinolinyl, a 1-meth...

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Hauptverfasser:	KRUPA MALGORZATA, RYZNAR TERESA, WINIARSKI JERZY, FITAK HANNA, CHODYNSKI MICHAL, KUTNER ANDRZEJ, SZELEJEWSKI WIESLAW, GORECKI BARTLOMIEJ
Format:	Patent
Sprache:	eng
Schlagworte:	ACYCLIC OR CARBOCYCLIC COMPOUNDS CHEMISTRY CLIMATE CHANGE MITIGATION TECHNOLOGIES IN THE PRODUCTION ORPROCESSING OF GOODS GENERAL TAGGING OF CROSS-SECTIONAL TECHNOLOGIES SPANNING OVER SEVERAL SECTIONS OF THE IPC GENERAL TAGGING OF NEW TECHNOLOGICAL DEVELOPMENTS METALLURGY ORGANIC CHEMISTRY TECHNICAL SUBJECTS COVERED BY FORMER USPC CROSS-REFERENCE ART COLLECTIONS [XRACs] AND DIGESTS TECHNOLOGIES OR APPLICATIONS FOR MITIGATION OR ADAPTATION AGAINSTCLIMATE CHANGE
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Beschreibung
Zusammenfassung:	Preparation of sulfonyl derivatives of cholecalciferol of Formula 1, wherein R1 is a protective group, preferably a t-butyl(dimethyl)silyl, and R2 is a heterocyclic group, such as a 2-thiazolyl, a 2-benzothiazolyl, a 1-phenyl-1H-tetrazo-5-yl, a 2-pyridyl, a 2-pyrimidynyl, a 1-isochinolinyl, a 1-methyl-2-imidazyl, or a 4-alkyl-1,2,4-triazo-3-yl, comprises the conversion of the hydroxyl derivative of cholecalciferol into the corresponding sulfide followed by its oxidation to the respective sulfone characterized by the use of a hydroxyl derivative of cholecalciferol as a starting material, in which the triene system is protected as a Diels-Alder adduct, and in particular as an adduct with sulfur dioxide of the Formula 2a. Novel are also the derivatives of Formula 3a and 4a, isolated in the process provided by the invention.