TETRAZOLO *A* QUINAZOLL55 ONES AS ANTIIALLERGIC AND ANTIITUMOR AGENT

摘要

1499255 Tetrazolo[a]-quinazolone derivatives PFIZER Inc 1 July 1976 [10 July 1975 28 Jan 1976] 27543/76 Heading C2C Novel compounds of the Formula I wherein each of R 1 and R 2 is hydrogen, halogen, C 1-4 alkyl, C 1-4 alkoxy, C 1-4 alkanoyloxy, benzyloxy, hydroxy, trifluoromethyl, or sulphonamide, or R 1 and R 2 when attached to adjacent carbon atoms in the ring and taken together form a methylenedioxy or ethylenedioxy group, provided R 1 and R 2 are not both hydrogen, and pharmaceutically acceptable cationic salts thereof, may be prepared by reacting the appropriate 2-chloro-4(3H)quinazolinone with a metal azide to form the tetrazole ring, optionally followed by debenzylating when R 1 and/or R 2 is benzyloxy to form the corresponding compound in which R 1 and/or R 2 is hydroxy and esterification of a free hydroxy group at R 1 and/or R 2 . The 2-chloro-4(3H)quinazolinones are prepared by reacting the appropriate anthranilic acid with urea or alkali metal isocyanate followed by heating to form a 2,4-(lH,3H)quinazolinedione, which with phosphorus oxychloride forms a 2,4-dichloroquinazoline which with base yields the required compound.