Patent ID: 6951937

Claim:
A process for preparing a compound of formula A: wherein R 1 is a member selected from the group consisting of: —CN, —O-methyl, —O-ethyl, —O-propyl, —O-isopropyl, —O-butyl, —O-t-butyl, —O-isoamyl, 1-naphthyloxy, 2-naphthyloxy, 4-indolyoxy, 5-inddolyoxly, 5-isoquinolyloxy; R 2 and R 4 are each independently a member selected from the group consisting of: hydrogen, —O—CH 3 , —O(—CH 2 )—CH 3 , —O(—CH 2 ) 2 —CH 3 , —O—CH 2 —CH═CH 2 , —O—CH 2 —C═CH and —O(—CH 2 ) n —R 3 ; wherein one of the R 2 and R 4 groups is —O(—CH 2 ) n —R 3 and the remaining R 2 or R 4 group is other than —O(—CH 2 ) n —R 3 ; n is 2 to 5; R 3 is a member selected from the group consisting of: piperidine, pyrrolidine, morpholine, piperazine, 4-methyl-piperidine and 2-methyl-piperidine, and all pharmaceutically acceptable isomers, salts, hydrates, solvates and N-acylated derivatives thereof, comprising the steps of: (a) etherifying the hydroxy group of a compound of formula I or its position isomer with a compound of formula II wherein L 1 is a leaving group, under basic etherification conditions in the presence of an appropriate solvent to produce a compound of formula III or its position isomer as follows: (b) nitrating the compound according to formula III, or its position isomer, to yield a compound according to formula IV, or its position isomer, at a suitable temperature in a solvent as follows: (c) reacting the compound of formula IV, or its position isomer, with an amine containing compound selected from the group consisting of piperidine, pyrrolidine, morpholine, piperazine, 4-methyl-piperidine and 2-methyl-piperidine, in the presence of a catalyst and a solvent to provide a compound of formula V, or its position isomer, as follows: (d) reducing the nitro group on the compound of formula V, or on its position isomer, to an amino group and thereby producing a compound of formula VI, or its position isomer, as follows: (e) reacting the compound of formula VI, or its position isomer with ammonium formate and formamide at a suitable temperature to produce a cyclized quinazoline derivative of formula VII, or its position isomer, as follows: (f) replacing the hydroxy group of the compound of formula VII, or its position isomer, with a leaving group Q to provide a compound of formula VIII, or its position isomer, as follows: (g) reacting the compound of formula VIII, or its position isomer, with a compound of the formula IX, or a salt thereof, to provide a compound of formula X, or its position isomer, as follows: (h) and optionally, producing a salt, solvate, hydrate, or N-acylated, of the compound of formula X, or its position isomer.