Synthesis and in vitro pharmacology of 7-oxabicyclo[2.2.1]heptane analogs of thromboxane A2/PGH2
作者:P. W. Sprague、J. E. Heikes、J. Z. Gougoutas、M. F. Malley、D. N. Harris、R. Greenberg
DOI:10.1021/jm00149a007
日期:1985.11
A series of chemically stable TXA2/PGH2 analogues modeled after the structure of the natural products was prepared in search of useful inhibitors of TXA2/PGH2-mediated pathophysiology. Each of the 16 isomers implied in structure 1 was prepared in chiral form and evaluated for activity in vitro in platelets and smooth muscle. Depending on relative side chain and carbinol stereochemistry, TXA2/PGH2 agonist
The application of thiazolium salt catalysed addition of aldehydes to α,β-unsaturated esters for the synthesis of the title compounds (1, 2 and 3) is discussed.
Notiz zur Synthese von (<i>E</i>)-12-Hydroxy-10-heptadecensäure, (5<i>E</i>, 10<i>E</i>)-12-Hydroxy-5, 10-heptadecadiensäure und (5<i>Z</i>, 10<i>E</i>)-12-Hydroxy-5,10-heptadecadiensäure
作者:Frank Kienzle
DOI:10.1002/hlca.19800630303
日期:1980.4.23
Note on the Synthesis of (E)-12-Hydroxy-10-heptadecenoic Acid, (5E, 10E)-12-Hydroxy-5, 10-heptadienoic Acid and (5Z, 10E)-12-Hydroxy-5,10-heptadienoic Acid