Abstract
The reaction of 8-phenyl-7-deazatheophyllines (I) with phosphorus oxychloride gave 6-chloro-6-deoxy-8-phenyl-7-deazatheophyllines (II) in high yields. Compounds II served as useful starting materials for several nucleophilic reactions. The reaction of I with phosphorus oxychloride in the presence of amines has been carried out to succeed in obtaining the corresponding 6-amino-derivatives in a single step. The reaction of 8-phenyl-theophylline (III) with phosphrous oxychloride gave 6-chloro-6-deoxy-8-phenyltheophylline (IV) in good yield. 6-Substituted 6-deoxy-8-phenyltheophyllines were prepared by the reaction of III with phosphorus oxychloride in the presence of amines in a single step. The reaction of I (or III) with phosphorus oxychloride essentially involves the conversion of aminoenketone (or aminoazadienketone) to iminoenchloride (or iminoazadienchloride).
