| 摘要 |
The penicillins I (A=phenyl, 4-hydroxyphenyl, 2-, 3-thi-enyl, phenyl radicals substituted at 3,4-positions; R=NH-Z-X; Z=C1-C6 straight or side chain alkylene, C3-C6 cycloalkyl substituted by X; X=cyano, hydroxy, mercapto, aminocarbonyl, aminosulfonyl) were prepd. Thus, 920mg 5-amino-2-(2'-methoxy-ethylamino)-4-hydroxypyrimidine was dissolved in 250mL anhyd. THF and mixed with 500mg NET3. This mixt. was added to 30mL THF contg. 500mg phosgen at 0≦̸C. Amoxillin3H2O was diffused with 80% THF and cooled at 0≦̸C. NET3 was added to the mixt., and maintained pH 7.5 within 5 min. After the prepn. was washed and acidified, the resulting ppt. was treated with Na-hexanoate and MeOH to give I.
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