Isothiazolyl substituted glycerol derivatives containing phosphate groups
Glycerol derivatives having at least one heterocyclic group on the 1 or 2 position are PAF antagonists which may be used to treat asthma, inflammation and shock.
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(2008/06/13)
An efficient synthesis of Platelet-Activating Factor (PAF) via 1-o-alkyl-2-o-(3-isoxazolyl)-SN-glycero-3-phosphocholine, a new PAF agonist utilization of the 3-isoxazolyloxy group as a protected hydroxyl
Potent PAF agonists (R)-3a,b were synthesized and converted into PAF. Key steps include Mitsunobu reaction of a chiral secondary alcohol with 3-hydroxyisoxazole as the acidic component, and hydrogenolytic ring cleavage of the resulting 3-isoxazolyloxy gro