Process for the synthesis of 1.alpha.,23(S),25-trihydroxycholecalciferol and 1.alpha.,23(R),25-trihydroxycholecalciferol
AssigneeHoffman-La Roche Inc.
InventorsEnrico G. Baggiolini, Milan R. Uskokovic, Peter M. Wovkulich
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Abstract
The invention is directed to a process and intermediates for the preparation of 1.alpha.,23(S),25-trihydroxycholecalciferol and 1.alpha.,23(R),25-trihydroxycholecalciferol. The end-products, 1.alpha.,23(S),25-trihydroxycholecalciferol and 1.alpha.,23(R),25-trihydroxycholecalciferol, are useful for the treatment of disease states which are characterized by insufficient amounts of 1,25 dihydroxycholecalciferol.
Claims22
A compound of the formula ##STR24## wherein R.sub.1 and R.sub.2 each independently are lower alkyl.
A compound of the formula ##STR25##
A compound of the formula ##STR26## wherein R.sup.4 is tri-lower alkylsilyl, di-lower alkylarylsilyl, lower alkyldiarylsilyl, triarylsilyl.
A compound of the formula ##STR27##
A compound of the formula ##STR28##
A compound of the formula ##STR29## wherein R.sup.1 and R.sup.2 each independently is hydrogen, lower alkyl or aryl, or taken together are lower alkylene of from 3 to 6 carbon atoms.
A compound of the formula ##STR30## wherein R.sup.1 and R.sup.2 each independently is hydrogen, lower alkyl or aryl or taken together are lower alkylene of from 3 to 6 carbon atoms.
A compound of the formula ##STR31##
Dependencies are inferred from the claim text.