| 摘要 |
Intermediates in drug development and preparation methods thereof are provided, thereby easily mass-producing the intermediates by performing their preparation under mild condition, so that clinical demonstration can be easily performed using intermediates mass-produced. The intermediates in drug development represented by formulas (1), (2), (3) and (4), pharmaceutically acceptable salts thereof, hydrates thereof and solvates thereof are provided, wherein the intermediate is selected from (S)-1-benzyl-pyrrolidin-3-ylamine, (s)-5-hydroxymethyl-1-methyl-pyrrolidin-(R)-3-ol, (S)-5-hydroxymethyl-pyrrolidin-2-one, and (R)-1-benzyl-pyrrolidin-3-ylamine. The method for preparing (S)-1-benzyl-pyrrolidin-3-ylamine comprises the steps of: preparing (S)-amino-succinic acid diethylester; preparing (S)-2-tert-butoxycarbonylamino succinic acid diethylester; preparing (S)-(3-hydroxy-1-hydroxymethyl-propyl)-carbamic acid tert-butylester; preparing (S)-methanesulfonic acid 3-tert-butoxycarbonylamino-4-hydroxy-butylester; preparing (S)-(1-benzyl-pyrrolidin-3-yl)-carbamic acid tert-butylester; and preparing (S)-1-benzyl-pyrrolidin-3-ylamine.
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