| 摘要 |
PROBLEM TO BE SOLVED: To simply obtain the above compound useful as an intermediate for medicines such as β-adrenergic nerve stimulating agent in a high yield and high quality. SOLUTION: An N-acylaniline derivative represented by formula II (e.g. 3-chloropropioneanisidine) is cyclized in the presence of an anhydrous aluminum chloride in a paraffin-based solvent (e.g. N,N-dimethylformamide) under heating to provide unsubstituted or 6-substituted 3,4-dihydrocarbostyril which is the objective compound represented by formula I (R is H, a halogen, a 1-4C alkoxy, etc.). As an amount of each reagent used in this reaction, the paraffin-based solvent is preferably used in an amount of 200-1000ml based on 100g compound of formula II and anhydrous aluminum chloride is preferably used in an amount of 4-7 times by mole based on the compound of formula II. |
