6-BETA-[BISTRIFLUOROMETHANESULFONYL]AMIDOPENICILLANIC ACID - A NOVEL BETA-LACTAMASE INHIBITOR

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作者
MEZES, PSF
FRIESEN, RW
VISWANATHA, T
DMITRIENKO, GI
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O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
Benzyl 6-.beta.-[bistrifluoromethanesulfonyl]amidopenicillanate, 4, was prepared by reaction of benzyl 6-.beta.-aminopenicillanate, 3, with 2 equivalents of trifluoromethane sulfonic anhydride. In the presence of aqueous base, 4 undergoes detriflation to yield 7 and in the presence of basic methanol, 4 yields the .alpha.-methoxymonotriflamide 6. The free acid 5 obtained by hydrogenolysis of 4 has [bacterial] .beta.-lactamase inhibitory properties.
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页码:1207 / 1210
页数:4
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