| 摘要 |
Diesters (I) [R=H, OH; R1=N3, NHCO2CH2C6H4R4; R2=Cl,Br,iodo; R3=H, Cl, Br, iodo; R4=H, Cl, Br, NO2, Me, MeO! and their pharm. acceptable acid addn. salts were prepd. Thus, 6,6-dibromopenicillanic acid was converted to its chloromethyl ester via its Bu4N+ salt. Chloromethyl 6.6-dibromopenicillanate was iodonated and oxidized to the 1,1- dioxide. Iodomethyl 6,6-dibromopenicillanate 1,1-dioxide was reacted with tetrabutylammonium 6-(D-2-azido-2-phenylacetamido)penicillanate to give I (R=H, R1=N3, R2=R3=Br), which was hydrogenate to I (R=H, R1=NH2, R2=R3=Br).
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