Abstract: The present invention relates to a process for preparing a protected 4-aminomethyl-pyrrolidin-3-one represented by the following formula (1) which is an essential intermediate for the preparation of quinolone antibiotics. wherein P1 and P2 independently of one another represent acetyl, t-butoxycarbonyl or pivaloyl, characterized in that a compound represented by the following formula (5): wherein P1 is defined as previously described, is reacted with a Raney-nickel catalyst in a solvent under hydrogen pressure to produce a compound represented by the following formula (6): wherein P1 is defined as previously described, in step 1; the amino group in the compound of formula (6) is protected to produce a compound represented by the following formula (7): wherein Pl and P2 are defined as previously described, in step 2, the double bond in the compound of formula (7) is selectively reduced by reacting the compound of formula (7) with a metal catalyst in a solvent under hydrogen pressure, and to novel intermediates of formulas (6) and (7) for preparing the compound of formula (1).
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| # | Name | Date |
|---|---|---|
| 1 | 349-del1999-form-1.pdf | 2011-08-21 |