Captagon,Homburg,W. Germany,1961
1 mol of 7-(β-chloroethyl)-theophylline and 2? mols of α-methyl-β-phenyl
ethylamine are heated for 6 hours in an oil bath, if necessary with addition of
alcohol or toluene. The reaction mixture is diluted with alcohol and acidified
with alcoholic hydrochloric acid. The crystalline mass formed is filtered with
suction and extracted by boiling with alcohol. A product having a melting point
of 237°C to 239°C is formed. With prolonged extraction by boiling with
alcohol, the melting point of the mass falls, preferably due to a change in
modification, to 227°C to 229°C. However, analysis shows that both products
are the pure condensation product.
Instead of the chloroethyl theophylline, it is also possible to use the
corresponding bromine derivative. It was found that in this way the process is
facilitated and the yield is improved