23,23-Difluoro-25-hydroxy-vitamin D.sub.3 and process for prepar

Details 23,23-Difluoro-25-hydroxy-vitamin D.sub.3 and process for prepar 23,23-Difluoro-25-hydroxy-vitamin D.sub.3 and process for prepar

1984-08-13

1986-01-14

Roberts, Elbert L.

Chemistry of carbon compounds

Miscellaneous organic carbon compounds

C-metal

26023955R, 2603971, C07J 900

Patent

active

045644748

ABSTRACT:
The invention provides new derivatives of vitamin D, 23,23-difluoro-25-hydroxycholecalciferol and the acylates thereof, a method for preparing said compounds and various new intermediates utilized in such process.
The derivative compounds are characterized by vitamin D-like activity as evidenced by their ability to increase intestinal calcium transport and serum calcium. The compounds are further characterized by resistance to hydroxylation at C-23, which is recognized as an essential metabolic step to the inactivation of vitamin D. The compounds should, therefore, provide vitamin D-like activity of greater time duration.

REFERENCES:
patent: 4196133 (1980-04-01), DeLuca et al.
patent: 4226788 (1980-10-01), DeLuca et al.
patent: 4397847 (1983-08-01), Boris et al.
Partridge et al., "Helvetica Chemica Acta.", vol. 57, Fasc 3 (1974), pp. 764-771.

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