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US 4,563,537 AGranted
Synthesis of thiophene-containing prostaglandin endoperoxide apparatus
AssigneeIowa State University Research Foundation, Inc.
InventorRichard C. Larock
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Abstract
New organopalladium reactions involving the addition of thienylpalladium compounds to strained bicyclic alkenes, and subsequent chain extension reactions employing the chemistry of organopalladium compounds are disclosed. By these techniques a large number of bicyclic prostaglandin analogs are prepared, which are useful as inhibitors of arachidonic acid induced blood platelet aggregation, and are specific inhibitors of thromboxane synthetase.
Claims6
Thiophene-containing prostaglandin endoperoxide analogs of the formula:
- ##STR21## wherein n equals a whole integer of from 0 to 7, X is carboxylic acid, or C.sub.1 -C.sub.8 ester, alcohol, ether or amide groups;
- Y is ethylene or cis or trans vinylene;
- A is methylene, ethylene, oxy, imino, or lower alkyl, phenyl or aryl substituted imino;
- D is methylene, ethylene, vinylene, methyleneoxy, alkylidenedioxy, iminooxy, dithio, or azo;
- B is ethylene, cis and trans vinylene, and ethynylene;
- R and R.sub.1 are hydrogen, lower alkyl and lower aryl or (CH.sub.2).sub.Z with Z being 2 to 5, and Q is hydroxy, methoxy, acetoxy or hydrogen, or Q and R.sub.1 are oxa.
3 more elements
A prostaglandin analog comprising:
- ##STR22## wherein R.sub.2 is selected from the group consisting of hydrogen and methyl.
Dependencies are inferred from the claim text.