Thiaprostaglandin E.sub.1 derivatives, process for production th

Details Thiaprostaglandin E.sub.1 derivatives, process for production th Thiaprostaglandin E.sub.1 derivatives, process for production th

1981-10-30

1984-08-21

Gerstl, Robert

Drug, bio-affecting and body treating compositions

Antigen, epitope, or other immunospecific immunoeffector

Recombinant or stably-transformed bacterium encoding one or...

424317, 424331, 424325, 560106, 560119, 560121, 560230, 562501, 562503, 564188, 564189, 568367, 568379, 556427, 548530, 546102, 546226, 544161, 544391, 542426, 549420, 549475, C07C17700, A61K 31557

Patent

active

044669801

ABSTRACT:
A novel compound selected from the group consisting of 7-(or 6- or 4-)thiaprostaglandin E.sub.1 derivatives of the formula (I). ##STR1## wherein A represents --CH.sub.2 -- or ##STR2## in which n is 0, 1 or 2, provided that only one A cut of three is ##STR3## R.sup.1 -R.sup.7 and G are as defined in the specification, the 15-epimers of said thiaprostaglandin E.sub.1 derivatives, the enatiomers of said thiaprostaglandin E.sub.1 derivatives or their 15-epimers, and mixtures of these compounds.
A 7-thiaprostaglandin E.sub.1 derivative and/or its optical isomer may be prepared by reacting a 2-organo-2-cyclopentenone (II) with an organic copper-lithium compound (III) to effect conjugation reaction. A 6-thiaprostaglandin E.sub.1 derivative and/or its optical isomer may be prepared by subjecting an .alpha.,.beta.-unsaturated ketone (IV) and a thiol (V) to the Michael addition reaction. And, 4-thiaprostaglandin derivative and/or its optical isomer may also be prepared by the Michael addition reaction from a 2-allyl substituted cyclopentanone (VI) and a thiol (VIII).
Some compounds ((I)-1) amongst the compounds of the formula (I) and/or their optical isomer are useful for controlling vascular actions such as angina pectoris, vasodilation etc.

REFERENCES:
patent: 4175201 (1979-11-01), Fried
patent: 4180672 (1979-12-01), Kurozumi
J. Org. Chem., vol. 40, 1975, pp. 521-523.
Tetrahedron Letters, No. 10, 1975, pp. 765-768.
Journal of Medicinal Chemistry, 1977, vol. 20, No. 12, pp. 1662-1665.
J. Am. Chem. Soc., 96, 1974, pp. 6759-6761.
Tetrahedron Letters, No. 48, 1974, pp. 4267-4270.
Tetrahedron Letters, No. 51/52, 1974, pp. 4459-4462.
Tetrahedron Letters, No. 52, 1976, pp. 4793-4796.
Tetrahedron Letters, No. 13, 1975, pp. 1165-1168.
Tetrahedron Letters, No. 19, 1977, pp. 1629-1632.

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