Process for preparing hypotensive 2-(4-aroylpiperazin-1-yl)-amino-6,7-dimethoxyquinazolines
AssigneePfizer Inc.
InventorPhilip D. Hammen
Life of this patent
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Abstract
Certain 2-(4-aroylpiperazin-1-yl)-4-amino-6,7-dimethoxyquinazolines are prepared by a novel process wherein certain 2-(4-substituted-piperazin-1-yl)-4-amino-6,7-dimethoxyquinazoline intermediates wherein said substituent is cyano, certain carbon-oxygen double bond containing groups or certain carbon-nitrogen double bond containing groups, are reacted with certain metalloaryl compounds followed by hydrolysis. The products are known hypotensive agents. Certain of the process intermediates are novel compounds.
Claims7
A process for preparing a product of the formula ##STR54## which comprises the steps of a. contacting one mole of a first reactant of the formula ##STR55## wherein R.sup.2 is a member selected from the group consisting of --CN, ##STR56## Y is a member selected from the group consisting of --OR.sup.3, --SR.sup.3 and --NR.sup.4 R.sup.5 ;
- R.sup.3 is a member selected from the group consisting of alkyl having from one to four carbon atoms and phenyl;
- R.sup.4 and R.sup.5 are the same or different and are each selected from the group consisting of alkyl having from one to four carbon atoms and phenyl;
- with from about one to three moles of a second reactant of the formula
- R.sup.1 M
- wherein R.sup.1 is a member selected from the group consisting of furyl, phenyl and thienyl;
- and M is a member selected from the group consisting of Li, Na and MgX where X is Cl, Br or I;
- under substantially anhydrous conditions in the presence of a reaction inert organic solvent at a temperature from about -80.degree. to 65.degree. C.;
- and
- b. hydrolyzing the reaction mixture obtained in step a.
Dependencies are inferred from the claim text.