Process for the preparation of 4-(4-(4-(hydroxybiphenyl)-1-piper

Details Process for the preparation of 4-(4-(4-(hydroxybiphenyl)-1-piper Process for the preparation of 4-(4-(4-(hydroxybiphenyl)-1-piper

1998-03-09

1999-11-23

Kight, John

Drug, bio-affecting and body treating compositions

Designated organic active ingredient containing

Having -c-, wherein x is chalcogen, bonded directly to...

546 22, 546239, 546241, C12P 1712

Patent

active

059901276

ABSTRACT:
The invention relates to the preparation of the compound 4-(4-(4-(hydroxydiphenyl)-1-piperidinyl)-1-hydroxybutyl)-.alpha.,.alpha.-d imethylphenylacetic acid and its phosphorylated derivatives. These compounds can be prepared from .alpha.-(p-tert-butylphenyl)-4-(.alpha.-hydroxy-.alpha.-phenylbenzyl)-1-pi peridinylbutanol with the aid of fungi of the genus Cunninghamella or Absidia. The compounds according to the present invention can be used as pharmaceuticals for the treatment of allergic disorders, allergic rhinitis or asthma. Compounds of the formula II in which R.sup.1 is --CH.sub.2 --O--P(O)(OH).sub.2 and R.sup.2 is --OH; R.sup.1 is --CH.sub.3 and R.sup.2 is --O--P(O)(OH).sub.2 ; or

REFERENCES:
patent: 4254129 (1981-03-01), Carr et al.
patent: 4285957 (1981-08-01), Carr et al.
patent: 5204249 (1993-04-01), Schwartz et al.
Patent Abstract of Japan, Band 15, No. 60 (C-805), Feb. 13, 1991; & JP 02-288883 A (Sankyo Co Ltd), Nov. 28, 1990.
H. Konzett et al., "Versuchsanordnung zu Untersuchungen an der Bronchialmuskulatur", Arch. Exp. Path. U. Pharmak., 195:71-74 (1940).
S. Schwartz et al., "Microbial Oxidation of Ebastine", Appl. Microbiol Biotechnol., 44:731-735 (1996).

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