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The preparation of two, preclinical amino-quinazolinediones as antibacterial agents

…, TT Curran, D Macikenas, RV Parlett IV…

文献索引：Beylin, Vladimir; Boyles, David C.; Curran, Timothy T.; Macikenas, Dainius; Parlett IV, Roger V.; Vrieze, Derek Organic Process Research and Development, 2007 , vol. 11, # 3 p. 441 - 449

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被引用次数: 18

摘要

This paper describes the synthesis of two amino-quinazolinediones which are potent gyrase/topoisomerase inhibitors and useful as antibacterial agents. The early scale-up work to prepare a chiral side chain on multigram scale and two different amino-quinazolinedione cores is detailed. The enabling synthesis for the side chain employed a previously reported Michael addition of MeNO2 to an enantiomerically enriched δ-amino-enoate and a two- ...

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