发明授权
US5589471A Vitamin D analogues containing a hydroxy or alkylated hydroxy group in the 20-position 失效
在20位含有羟基或烷基化羟基的维生素D类似物

Vitamin D analogues containing a hydroxy or alkylated hydroxy group in
the 20-position
摘要:
Compounds of formula ##STR1## wherein Q is a --CH.sub.2 --, --CH.dbd.CH-- or --C.dbd.C--; U is a C.sub.1 -C.sub.6 alkylene; R.sup.1 is hydrogen, a C.sub.1 -C.sub.4 alkyl or YR' in which Y stands for the radicals --SO-- or --SO.sub.2 -- and R' stands for a C.sub.1 -C.sub.4 alkyl; R.sup.2 and R.sup.3 are independently hydrogen or C.sub.1 -C.sub.4 alkyl, and additionally R.sup.2 and R.sup.3, when taken together with the starred carbon atom, may form a C.sub.3 -C.sub.6 carbocyclic ring; Z is hydrogen or hydroxy; and derivatives thereof. The compounds show antiinflammatory and immunomodulating effects as well as strong activity in inducing differentiation and inhibiting undesirable proliferation of certain cells. The compounds are prepared by adding an anion R.sup.- to 1(S),1(R)-bis-(tert-butyldimethylsilyl-oxy)-9,10-secopregna-5(E),7(E),10(19)-triene-20-one and the resulting compound is alkylated or acylated with R.sup.1 X.sup.1 where X.sup.1 is a leaving group followed by triplet-sensitized photoisomerization and deprotection to give the compound of formula I.
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