http://rdf.ncbi.nlm.nih.gov/pubchem/patent/US-2010222614-A1

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filingDate 2010-01-11-04:00^^<http://www.w3.org/2001/XMLSchema#date>
inventor http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_aaa887f491e389d2b957d16076898ada
http://rdf.ncbi.nlm.nih.gov/pubchem/patentinventor/MD5_26eddb53a4178a7a62eac22b047a1867
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publicationDate 2010-09-02-04:00^^<http://www.w3.org/2001/XMLSchema#date>
publicationNumber US-2010222614-A1
titleOfInvention Process for the preparation of calcipotriol
abstract A process for the preparation of calcipotriol at least including: (a) reacting a C-22 phenylsulfonyl derivative of cholecalciferol of Formula 2, wherein R 1 and R 2 are the same or different and represent hydroxyl protecting groups, with a silyl derivative of alfa-hydroxy aldehyde of Formula 3, wherein R 3 represents silyl group of formula Si(R 4 )(R 5 )(R 6 ), where R 4 -R 6 are the same or different and represent C 1-6 alkyl or phenyl groups, in the presence of a strong organic base in an aprotic solvent, followed by reductive desulfonation of the obtained diastereomeric mixture of alfa-hydroxysulfones with sodium amalgam, removal of the hydroxyl protecting groups, and purification of the product. The process leads to the formation of calcipotriol containing less than 0.3% of the (22Z)-isomer. The obtained calcipotriol is free of mercury traces.
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