Synthesis of 1.alpha.,25-dihydroxy-24R-fluorocholecalciferol and

Details Synthesis of 1.alpha.,25-dihydroxy-24R-fluorocholecalciferol and Synthesis of 1.alpha.,25-dihydroxy-24R-fluorocholecalciferol and

1984-04-11

1987-01-06

Schenkman, Leonard

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

9,10-seco- cyclopentanohydrophenanthrene ring system doai

2603972, A61K 3159

Patent

active

046346929

ABSTRACT:
1.alpha.,25-Dihydroxy-24R-fluorocholecalciferol and 1.alpha.,25-dihydroxy-24S-fluorocholecalciferol, analogs of 1.alpha.,25-dihydroxy-cholecalciferol which is physiologically the most active metabolite of vitamin D.sub.3, are synthesized in a multistep process from the known substance 1.alpha.,3.beta.-dihydroxyandrost-5-en-17-one. The new analogs are characterized by the ability to increase intestinal calcium transport, increase serum calcium and phosphate concentrations and to increase the deposition of these minerals in bones. These compounds will find a ready application as substitutes for natural 1.alpha.,25-dihydroxycholecalciferol in the treatment of disease states characterized by metabolic calcium and phosphate deficiencies. Exemplary of such disease states are the following: osteomalacia, osteoporosis, rickets, osteitis fibrosa cystica, renal osteodystrophy, osteosclerosis, anti-convulsant treatment, osteopenia, fibrogenesis-imperfecta ossium, secondary hyperparathyrodism, hypoparathyroidism, hyperparathyroidism, cirrhosis, obstructive jaundice, drug induced metabolism, medullary carcinoma, chronic renal disease, hypophosphatemic VDRR, vitamin D-dependent rickets, sarcoidosis, glucocorticoid antagonism, malabsorption syndrome, steatorrhea, tropical sprue, idiopathic hypercalcemia and milk fever.

REFERENCES:
patent: 4069321 (1978-01-01), Jones et al.
patent: 4098801 (1978-07-01), Micheli
patent: 4305880 (1981-12-01), DeLuca et al.
patent: 4358406 (1982-11-01), DeLuca et al.
patent: 4435325 (1984-03-01), Holly et al.
Chem Abstracts, 93:239788v, Japan Kokai Tokkyo Koho, 80 76,858.

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