| 摘要 |
<p>PURPOSE: Provided is a method for preparation of protected 4-aminomethyl-pyrrolidone-3-on represented by the formula(1) efficiently, which is an intermediate being essential in synthesizing quinolone based antibiotics. CONSTITUTION: The method for preparing protected 4-aminomethyl-pyrrolidone-3-on represented by the formula(1) is composed of the following steps of: (a) reacting a compound represented by the formula(5) with LaNi-nickel catalyst under hydrogen pressure in solvent, to obtain a compound represented by the formula(6); (b) reacting an amino group of the compound represented by the formula(6) with a protection group in the presence of base in solvent, to obtain a compound represented by the formula(7); and (c) reacting a compound represented by the formula(7) with metallic catalyst under hydrogen pressure in solvent, thus reducing double bond selectively, to obtain a compound represented by the formula(1), wherein P1 and P2 mean acetal, t-butoxycarbonyl or pivaloyl, respectively.</p> |
