Oxiranes

Details Oxiranes Oxiranes

1989-11-01

1990-08-14

Springer, David B.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

549551, 549554, 549556, C07D40510, C07D3038, C07D30312

Patent

active

RE0333000

ABSTRACT:
There are described compounds of formula ##STR1## in which n is 0, 1 or 2, R.sup.1 is a hydrocarbyl group optionally substituted with an optionally substituted phenyl group and containing from 5 to 30 carbon atoms, R.sup.2 is optionally substituted phenyl or C.sub.1-10 alkyl optionally substituted by one or more substituents selected from optionally protected hydroxyl, optionally protected carboxyl, nitrile, optionally protected tetrazolyl, --COR.sup.6 where R.sup.6 is C.sub.1-4 alkyl, C.sub.1-4 alkoxy, an optionally protected amino acid residue or --NR.sub.2.sup.7 where each R.sup.7 is hydrogen or C.sub.1-4 alkyl, and --NHR.sup.8 where R.sup.8 is hydrogen, a protecting group, an optionally protected amino acid residue, C.sub.1-4 alkyl or --COR.sup.9 where R.sup.9 is C.sub.1-4 alkyl or C.sub.1-4 alkoxy, and R.sup.3, R.sup.4 and R.sup.5 are each selected from hydrogen, carboxyl, C.sub.2-5 alkoxycarbonyl, C.sub.1-4 alkyl, C.sub.1-4 alkoxy, hydroxyl, optionally protected tetrazolyl, halo, trifluoromethyl, nitrile, nitro and --CONR.sub.2.sup.10 where each R.sup.10 is hydrogen or C.sub.1-4 alkyl; and salts thereof. The compounds are leukotriene antagonists.

REFERENCES:
Prelog, V. et al, Helv. Chem. Acta, 27, 1209 (1944) Chem. Abstracts 40:848(8).
Russell, G. A. et al., J. Org. Chem. 31(9) 2854 (1966).
Kano, S. et al, J.C.S. Chem Comm 785 (1978).
Eberbach et al., Chem. Ber., 114, 2979 (1981).
Eberbach et al., Tetrahedron Letters, (48) 4649 (1979).
Tamura et al., Synthesis, (10), 693 (1977).
Braun et al., Tetrahedron Letters, 41, 4033 (1973), p. 4035.

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