Process for the preparation of bispyrrolinyl derivatives of phenothiazines, phenoxazines and acridans

摘要

Bispyrrolinyl derivatives of phenothiazines, phenoxazines and acridans are obtained by reacting a phenothiazine, phenoxazine or acridan with a pyrrolidinone in the presence of phosphorus oxychloride. The phenothiazine, phenoxazine or acridan can likewise be converted by alkylation with 2-chloro-1-(1-pyrrolin-2-yl)-2-pyrroline into the required compounds. Typical examples of these bispyrrolinyl derivatives are 2-methoxy-10-[5-methyl-1-(5-methyl-1-pyrrolin-2-yl)-2-pyrrolin-2-yl]-p henothiazine, 10-[1-(1-pyrrolin-2-yl)-2-pyrrolin-2-yl]phenoxazine and 9,9-dimethyl-10-[5-methyl-1-(5-methyl-1-pyrrolin-2-yl)-2-pyrrolin-2-yl ]acridan. The amidine compounds can be used as diuretics, smooth muscle relaxants and antithrombogenic agents.