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85030900759
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note
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Coupling glycine ethylester hydrochloride with ethyl acrylate in the presence of triethylamine, Cbz protection and potassium tert-butoxide assisted cyclization can give the indicated starting material 1 (1-benzyl 3-ethyl 4-oxo-1,3-pyrrolidinedicarboxylate).
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14
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85030902111
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note
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All cultures were obtained from Hoechst and MICs were determined by the agar dilution method as recommended by the National Committee for Clinical Laboratory Standards.
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15
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85030905961
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note
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14: 7-(3-Aminomethyl-4-methoxyimino-3-methyl-piperidin-1-yl)-1- cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid hydrochloride, 15: 7-(3-Aminomethyl-4-benzyloxyimino-3-methyl-pyrrolidin-1-yl)- 1-cyclopropyl-6-fluoro-4-oxo-1,4-dihydro-[1,8]naphthyridine-3-carboxylic acid hydrochloride, 16: 7-(4-Aminomethyl-4,8,8-trimethyl-7,9-dioxa-2-aza-spiro[4.5] dec-2-yl)-1-cyclopropyl-6-fluoro-4oxo-1,4-dihydro-[1,8]naphthyridine-3- carboxylic acid hydrochloride.
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16
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85030909428
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note
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3, Radiation=Mo Kα(λ=0.71069), Space group=P1, Z=2, Final R=0.0793.
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17
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85030907350
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note
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2O, 25°C).
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18
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0020411041
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