Theophylline has been used for decades to treat both acute and chronic asthma. However, in practice, theophylline is not a particularly easy drug to use because of its physical and pharmacological properties. It is poorly soluble in water; furthemore, it is frequently associated with gatric upset and palpitations. One of the theophylline derivatives that has been used in an attempt to circumvent side effects is acefylline (theophylline-7-acetic acid). Acefylline was synthesized by Baisse in 1949[1] and is currently marketed as an alternative to theophylline. However, The raw material for domestic pharmaceutical production is now mainly imported, so acefylline was synthesized. The Optimal yield obtained when the reaction is carried out at 90oC, mol ratio theofylline: chloroacetic acid:NaOH = 1:1,6:2,9. Its structure was confirmed by FTIR, MS, 1H NMR and 13C NMR spectral data. The product has very high purity rate (99.97% by HPLC) and can be used as a pharmaceutical ingredient.
