| 摘要 |
PURPOSE:To obtain a pyrrolidine derivative substituted at 3-position containing a novel substance useful as an intermediate for synthesizing a penem derivative, etc. having improved antibacterial action inexpensively and easily in high yield, by reacting a specific 1,2,4-trisubstituted butane derivative with NH3. CONSTITUTION:A 1,2,4-trisubstituted butane derivative shown by the formula II(X<1> and X<2> are nucleophilic releasable group such as alkylsufonyloxy, etc.; Y is OH, protected OH, alkylsulfonyloxy, trihalogenoalkylsulfonyloxy, arylsulfonyloxy, or halogen) is reacted with NH3 in an inert solvent optionally in the presence of a base at room temperature -100 deg.C for 10min -several days to give the desired compound shown by the formula I (Y is acyloxy, lower alkylsufonyloxy, arylsulfonyloxy, novel substance when Y is Br) or its salt useful as an intermediate for synthesizing a 3-methyl-mercaptopyrrolidine derivative useful as an important intermediate for synthesizing a penem derivative, etc.
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