The invention discloses a simple and direct method for synthesizing pyridine monoamine and its derivatives. Pyridine monoamine and its derivatives have a structural formula as shown in formula (I). The preparation comprises the steps of: reacting the main materials of trisubstituted alkene shown in formula (II) with isocyanide shown in formula (III) in the presence of the catalyst alkali in an organic solvent under a certain temperature condition so as to obtain the target product. The method for synthesizing pyridine monoamine and its derivatives in the invention has simple operations and mild reaction conditions, and can generate products of good biological activity. And the (I), (II) and (III) have the following structural formulas.