| 摘要 |
2-AMinobenzylamines (I): (where Hal = Cl or Br; R1 = H, Cl or Br; R2 = cyclohexyl, hydroxycyclohexyl, morpholinocarbonylmethyl or isopropylaminocarbonylmethyl gp.; R3 = H or methyl and R4 = H, or, if R2 = isopropylaminocarbonylmethyl or morpholinocarbonylmethyl gp., a benzoyl gp., are made by reacting an aldehyde (II): with an amine HN(R2)(R3) in the presence of formic acid or the corresp. formamide at elevated temps. and, if R2 in the amine = H, subsequently refluxing the reaction mixt. with a dil. acid. The process gives higher yields than known reductive amination processes using formic acid. The prodts. have useful pharmacological props., esp. secretolytic, pectoral and respiratory props. |
