Fluorine derivatives of vitamin D.sub.3 and process for producin

Details Fluorine derivatives of vitamin D.sub.3 and process for producin Fluorine derivatives of vitamin D.sub.3 and process for producin

1987-10-14

1989-08-01

Robinson, Douglas W.

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

9,10-seco- cyclopentanohydrophenanthrene ring system doai

2603972, A61K 3159, C07J 900

Patent

active

048533785

ABSTRACT:
There are disclosed novel derivatives of 26,26,26,27,27,27-hexafluorovitamin D.sub.3 having fluorine atom at the 23- and/or 24-position which have an excellent pharmacological activity and a process for production thereof. The novel compounds are represented by the general formula: ##STR1## wherein R.sub.1 ' denotes a hydrogen atom, a hydroxyl group or a protected hydroxyl group, R.sub.2 denotes a hydrogen atom or a protecting group for hydroxyl group, R.sub.3 denotes a hydrogen atom, a fluorine atom, a hydroxyl group or a protected hydroxyl group and R.sub.4 and R.sub.4 ' each denotes a hydrogen atom, or one of them denotes a hydrogen atom and the other denotes a fluorine atom, hydroxyl group or a protected hydroxyl group or R.sub.4 and R.sub.4 ' are combined to denote an oxo group, with a proviso that at least one of R.sub.3, R.sub.4 and R.sub.4 ' denote a fluorine atom. The process for production thereof comprises subjecting to thermal isomerization a compound represented by the general formula: ##STR2## wherein R.sub.1 ', R.sub.2, R.sub.3, R.sub.4 and R.sub.4 ' are the same as defined above, to thermal isomerization and optionally further to deprotection reaction.

REFERENCES:
patent: 4201881 (1980-05-01), Deluca
patent: 4248791 (1981-02-01), Deluca et al.
patent: 4305880 (1981-12-01), Deluca et al.
patent: 4358406 (1982-11-01), Deluca et al.
patent: 4495181 (1985-01-01), Norman et al.
patent: 4552698 (1985-11-01), Deluca
Chemical Abstracts, vol. 106, No. 19, May 11, 1987, p. 4, Abstract No. 156774y.
Chemical Abstracts, vol. 106, No. 11, Mar. 16, 1987, p. 643, Abstract No. 84955h.
Chemical Abstracts, vol. 102, No. 1, Jan. 7, 1985, p. 549, Abstract No. 6060r.
Chemical Abstracts, vol. 103, No. 15, Oct. 14, 1985, p. 83, Abstract No. 116282t.
Chemical Abstracts, vol. 104, No. 20, May 19, 1986, p. 391, Abstract No. 174464a.
Proceeding of the National Academy of Sciences, vol. 80, Jan. 1983, pp. 201-204, Y. Honma et al.
Pharm. Soc. Japan, 105 th Annual Meeting, Abstracts of Speeches, p. 621, No. 404-1 (1985).

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