STRUCTURE-ACTIVITY-RELATIONSHIPS IN THE 2-ARYLCARBAPENEM SERIES - SYNTHESIS OF 1-METHYL-2-ARYLCARBAPENEMS

STRUCTURE-ACTIVITY-RELATIONSHIPS IN THE 2-ARYLCARBAPENEM SERIES - SYNTHESIS OF 1-METHYL-2-ARYLCARBAPENEMS
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DOI:
10.1021/jm00388a022
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发表时间:
1987-05-01
影响因子:
7.3
通讯作者:
CHRISTENSEN, BG
CHRISTENSEN, BG
中科院分区:
医学1区
文献类型:
--
作者:
GUTHIKONDA, RN;CAMA, LD;CHRISTENSEN, BG

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氮杂环丁烷酮6-8b的不稳定的叔丁基二甲基甲硅烷基酯在制备潜在有用的叶立德吡啶基硫代酯18-20中充当关键的配体。利用这些中间体合成了一系列标题碳青霉烯类化合物25- 30 d、32和49-53。这些碳青霉烯类抗生素的抗菌性能和DHP-I的敏感性进行了研究,参考硫霉素。
The labile tert-butyldimethylsilyl esters of the azetidinones 6-8b served as the crucial synthons in the preparation of the potentially useful ylide pyridyl thio esters 18-20. These intermediates were utilized to synthesize a host of title carbapenems 25-30d, 32, and 49-53. The antimicrobial properties and DHP-I susceptibility of these carbapenems were studied with reference to thienamycin.