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Improved Synthetic Routes to the Novel Thromboxane Receptor Antagonist ICI 192605: Activity of Synthetic 1,3-dioxane Intermediates

Improved Synthetic Routes to the Novel Thromboxane Receptor Antagonist ICI 192605: Activity of Synthetic 1,3-dioxane Intermediates

G R Brown, A J Foubister, J A Hudson

J Pharm Pharmacol. 1990 Jan;42(1):53-5.

PMID: 1969951

Abstract:

A study of the synthetic routes to the thromboxane receptor antagonist ICI 192605 4(Z)-6-(2-o-chlorophenyl-4-o-hydroxyphenyl-1,3-dioxan-cis-5-yl) hexenoic acid is described which led to an improvement in overall synthetic yield from 20 to 55%. Invitro thromboxane receptor antagonist data are reported for the novel 1,3-dioxane synthetic intermediates. These data indicated that shortening of the side chain in an appropriately substituted 2,2-dimethyl-1,3-dioxane (e.g. ICI 180080) from a heptenoic acid, to a hexenoic acid, had little effect on thromboxane receptor antagonist potency (pA2 = 7.5 rabbit thoracic aorta for the heptenoic acid ICI 180080 and pA2 = 6.9 for the corresponding hexenoic acid. Human platelet aggregation pA2 values were 6.7 and 7.0, respectively).

Chemicals Related in the Paper:

Catalog Number	Product Name	Structure	CAS Number	Price
AP117621644	ICI 192605		117621-64-4	Price

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