abstract |
NEW MATERIAL: A compd. represented by formula I [X is R 2 (R 2 is 1-25C alkyl), H, halogen or -CO 2 R 3 (R 3 is 1-25C alkyl), R 1 is H, 1-25C alkyl, 1-5C alkoxy or halogen, Y is a 5- 7-membered mono-- di-cyclic aromatic heterocycle which contains an N atom bonded to a methylene group and may contain an atom other than N and S and n is 0 or 1]. n EXAMPLE: 3-[[3-[[[3-(hexadecyloxy)-2-methylphenoxy] hydroxyphosphynyl]oxy]phenyl]methyl]thiazolium, hydroxide, internal salt. n USE: A bis-arylphosphate ester antagonist of a platelet activating factor. Useful for treating asthma, anaphylaxis, a shock of sepsis and psoriasis. n PREPARATION: Alcohol represented by formula II is treated with an equivalent of phosphorus reagent represented by formula III (J is a leaving group) to form phosphate represented by formula IV and this compd. is reacted with a nitrogen- containing heterocyclic compd. n COPYRIGHT: (C)1990,JPO |