| abstract |
A method of synthesizing 4- [3- (4-cyclopropanecarbonyl-piperazine-1-carbonyl) -4-fluorobenzyl] -2H-phthalazin-1-one from 2-carboxybenzaldehyde, comprising the steps of: (a) synthesizing Diethyl 3-oxo-1,3-dihydro-2-benzofuran-1-yl) phosphonate from 2-carboxybenzaldehyde; (b) synthesize 2-fluoro-5 - [(E / Z) - (3-oxo-2-benzofuran-1 (3H) -ylidene) methyl] benzonitrile from (3-oxo-1,3-dihydro- Diethyl benzofuran-1-yl) phosphonate; (c) synthesize 2-fluoro-5 - [(4-oxo-3,4-dihydroftalazin-1-yl) methyl] benzonitrile from 2-fluoro-5 - [(E / Z) - (3-oxo- 2- benzofuran-1 (3H) -ylidene) methyl] benzonitrile by reaction with hydrazine hydrate; (d) synthesize 2-fluoro-5- (4-oxo-3,4-dihydro-phthalazin-1-ylmethyl) -benzoic acid from 2-fluoro-5 - [(4-oxo-3,4-dihydroftalazin -1-yl) methyl] benzonitrile by reaction with sodium hydroxide; (e) reacting 2-fluoro-5- (4-oxo-3,4-dihydro-phthalazin-1-ylmethyl) -benzoic acid with 1- (cyclopropylcarbonyl) piperazine or a mineral acid salt thereof in the presence of an amide coupling agent. |