Towards the synthesis of fluoro-thromboxane A₂ analogues

Abstract

Firstly, the biosynthesis and physiological role of thromboxanes and the potential for a thromboxane A₂ antagonist in cardiovascular therapy are discussed. Secondly, the importance of fluorine in drug design is outlined and the syntheses of a series of thromboxane A₂ structural analogues are reviewed. This is concluded by proposing how fluorine substitution should allow synthesis of a stable structural analogue of thromboxane A₂ which may have antagonistic properties. Finally, the synthetic conversion of a carbohydrate precursor, levoglucosan, into a suitable precursor to 10-α-flurothromboxane A₂ is discussed in detail.