1,2,9,10-Tetramethoxy-aporphin cough remedy prepn. - by reacting 1,10-di:methoxy-2,9-di:hydroxy-aporphin with phenyl-tri:methyl-ammonium hydroxide, methoxide or ethoxide

摘要

The prepn. of D(+)1,2,9,10-tetramethoxyaporphin (I) comprises (a) reacting 1,10-dimethoxy-2,9-dihydroxyaporphin (II) with phenyltrimethylammonium hydroxide, methoxide or ethoxide for 1/2-2 hrs. at 100-120 deg.C; (b) acidifying the product with an acid; (c) sepg.the pptd. N,N-dimethylaniline by-product; opt. (d) washing the soln. with an organic solvent; and (e) making the soln. basic and sepg. the pptd (I). (I) can be used as an anti-cough agent with adrenolytic properties and cough inhibiting activity superior to those of the known cough remedy codein. (I) is no intoxicant and is not addictive. (I) is obtd. in a single stage process in almost quantitative yields. The reactants are readily available and are not difficult to work with.