1581683-57-9Relevant articles and documents
Preparation method of 2-(2-(tert-butyloxycarbonyl)-2-azaspiro [3.4] octane-5-yl) acetic acid
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Paragraph 0035-0037; 0041; 0046-0048; 0052; 0057-0059; 0062, (2021/03/30)
The invention discloses a preparation method of 2-(2-(tert-butyloxycarbonyl)-2-azaspiro [3.4] octane-5-yl) acetic acid. The preparation method comprises the following steps: dissolving a compound 1 and a compound 2 in 2-methyl tetrahydrofuran, dropwise adding lithium bis (trimethylsilyl) amide, and reacting to obtain a compound 3; dissolving the compound 3 into acetone, and reacting with sodium iodide to obtain a compound 4; dissolving the compound 4 in 2-methyl tetrahydrofuran, dropwise adding n-butyllithium, and reacting to obtain a compound 5; dissolving the compound 5 into 2-methyl tetrahydrofuran, then adding a compound 6, alkali and 1, 8-diazabicyclo undecene-7-ene, and reacting at room temperature to obtain a compound 7; dissolving the compound 7 into ethyl acetate, adding a catalyst, and reacting in hydrogen to obtain a compound 8; dissolving the compound 8 into tetrahydrofuran and water, adding alkali for hydrolysis to obtain a final compound 9, and continuously optimizing thestructure of a spiro compound to obtain the synthesis method suitable for industrial production.
TRICYCLIC GYRASE INHIBITORS FOR USE AS ANTIBACTERIAL AGENTS
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Paragraph 0286; 0288; 0289, (2014/04/03)
Disclosed herein are compounds having the structure of Formula I and pharmaceutically suitable salts, esters, and prodrugs thereof that are useful as antibacterially effective tricyclic gyrase inhibitors. In addition, species of tricyclic gyrase inhibitors compounds are also disclosed herein. Related pharmaceutical compositions, uses and methods of making the compounds are also contemplated.