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|Title:||Process for the preparation of tetrahydropyrimidoisoindolols|
|Abstract:||This invention is concerned with tetrahydropyrimidinyl phenyl carbonyl acid addition salts, imidazolinyl phenyl carbonyl acid addition salts, dihydroimidazoisoindolols, tetrahydropyrimidoisoindolols, and tetrahydropyrimidoisoindolol acid addition salts which are all pharmacologically efficacious as anti-depressants. The tetrahydropyrimidinyl phenyl carbonyl acid addition salts, the tetrahydropyrimidoisoindolols and the tetrahydropyrimidoisoindolol acid addition salts are also efficacious as diuretics while the imidazolinyl phenyl carbonyl acid addition salts and the dihydroimidazoisoindolols are efficacious as anorexiants. This invention is also concerned with several processes for the preparation of these compounds.|
|Inventor(s):||Sulkowski; Theodore S. (Wayne, PA)|
|Assignee:||American Home Products Corporation (New York, NY)|
|Filing Date:||Sep 05, 1973|
|Claims:||1. A process for the preparation of a compound having the formula: ##SPC7## wherein R.sub.1 is selected from the group consisting of hydrogen, lower alkyl, phen(lower)alkyl, phenyl, monohalophenyl, dihalophenyl, mono(lower)alkylphenyl, di(lower)alkylphenyl, trifluoromethylphenyl, mono(lower)alkoxyphenyl, di(lower) alkoxyphenyl, thienyl, pyridyl, furyl and tetrahydro-2-naphthyl; R.sub.2 is selected from the group consisting of hydrogen, halogen, amino, lower alkylamino, lower alkyl and lower alkoxy; wherein said lower alkyl and said lower alkoxy have from one to six carbon atoms and R.sub.3 is hydrogen when R.sub.2 and R.sub.3 are dissimilar; and when R.sub.2 and R.sub.3 are the same they are both selected from the group consisting of hydrogen, halogen, lower alkyl and lower alkoxy wherein said lower alkyl and said lower alkoxy have from one to six carbon atoms which comprises the step of contacting a compound selected from the group consisting of those having the formula: ##SPC8## |
wherein R.sub.1, R.sub.2 and R.sub.3 are defined as above, in a reaction inert solvent, with an oxidizing agent selected from the group consisting of gaseous oxygen, potassium dichromate, potassium chlorate and hydrogen peroxide.
2. A process as described in claim 1 wherein the oxidizing agent is gaseous oxygen.
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