| 摘要 |
PURPOSE:To obtain the subject compound useful as an intermediate for synthesizing cerebral function disorder-improving medicines by reacting an aminonitrile derivative with a ketone derivative in the presence of a strong acidic ion exchange resin and subsequently reacting the reactional product with a Lewis acid. CONSTITUTION:A compound of formula I (A forms a five-six membered carbon ring or heterocyclic ring together with C) is reacted with a compound of formula II (B forms a five-six membered ring together with C) in the presence of a strong acidic ion exchange resin (e.g. Amberlist 15, Rohm & Haas Inc) in a solvent (e.g. 1,2-dichloroethane) at the refluxing temperature of the reaction mixture, and further reacted with a Lewis acid (e.g. anhydrous zinc chloride) preferably under an azeotropic dehydration treatment to provide the objective compound of formula III, e.g. 4-amino-2,3-dimethyl-5,6,7,8-tetrahydro-furo[2,3- b]quinoline. The compound of formula II, the catalyst and the Lewis catalyst are used in amounts of 0.5-10 equivalents, 0.1-50wt.% and 0.1-10 equivalents, respectively, based on the amount of the compound of formula I. |
