Process for preparing benzodiazepines
AssigneeHoffmann-La Roche Inc.
InventorGeorge Oswald Chase
Life of this patent
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Abstract
1,4-Benzodiazepin-2-ones are prepared via the reaction of a haloacetamidophenyl ketone with hexamethylenetetramine in the presence of ammonia. The 1,4-benzodiazepin-2-ones so prepared are known compounds useful as muscle relaxant and anti-convulsant agents.
Claims16
A process for preparing a compound of the formula ##STR9## wherein D is selected from the group consisting of ##STR10## R.sub.1 is selected from the group consisting of hydrogen, halogen, nitro and trifluoromethyl;
- R.sub.2 is selected from the group consisting of hydrogen and lower alkyl;
- and R.sub.3 is selected from the group consisting of hydrogen and halogen
- which comprises reacting a compound of the formula ##STR11## wherein D, R.sub.1 and R.sub.2 are as above and X is selected from the group consisting of chlorine, bromine and iodine
- with hexamethylenetetramine in the presence of ammonia and an inert organic solvent.
A process for preparing a compound of the formula ##STR14## wherein D is selected from the group consisting of ##STR15## R.sub.1 is selected from the group consisting of hydrogen, halogen, nitro and trifluoromethyl;
- R.sub.2 is selected from the group consisting of hydrogen and lower alkyl;
- and R.sub.3 is selected from the group consisting of hydrogen and halogen
- which comprises reacting a compound of the formula ##STR16## wherein D, R.sub.1 and R.sub.2 are as above and X is selected from the group consisting of chlorine, bromine and iodine
- with formaldehyde in the presence of ammonia and an inert organic solvent.
Dependencies are inferred from the claim text.