摘要 |
PROBLEM TO BE SOLVED: To provide a method of producing (2S,4R)-2-dimethylaminocarbonyl-4-methanesulfonyloxy-1-p-nitrobenzyloxycarbonylpyrrolidine (3) with simple manipulation in a high yield. SOLUTION: Trans-1-p-nitrobenzyloxycarbonyl-4-hydroxy-L-proline (1) is reacted with 2.5 or more equivalence of methanesulfonic chloride in the presence of a base and then reacted with a dimethylamine while an increased temperature of the reactant is controlled 4°C or lower. COPYRIGHT: (C)2008,JPO&INPIT
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