Metal [beta]-lactamase inhibitor cyclo-amidodithioformate derivative and preparation method of same
A cyclic aminodithioformate and lactamase technology, applied in organic chemistry, antibacterial drugs, etc., can solve the problems of difficult treatment, wide drug resistance spectrum, poor sensitivity, etc., to achieve Develop promising effects
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Embodiment 1
[0042] The preparation of embodiment 1 compound 1a
[0043] At room temperature, take the compound anhydrous piperidine (100mg, 1.16mmol) and sodium hydroxide (93mg, 2.32mmol) into a 10mL single-necked bottle, add 2mL of ethanol, stir at room temperature, the system is not completely dissolved; add carbon disulfide (169μL, 2.79 mmol), the system turns golden white and turbid, and the reaction stops in about half an hour. The solvent was distilled off under reduced pressure, an appropriate amount of ethyl acetate was added, the solid adhering to the bottle wall was scraped off with a spoon, filtered with suction, the filter cake was rinsed with ethyl acetate again, and vacuum-dried to obtain 325 mg of white solid with a yield of 99%.
[0044] m.p.: >300°C; 1 H NMR (400MHz,D 2 O)δ4.38(s,1H). 13 C NMR (100MHz,D 2 O) δ209.13,50.21.
Embodiment 2
[0045] The preparation of embodiment 2 compound 2a
[0046] At room temperature, the compound 1,4,7-triazacyclononane was taken in a solvent, and the preparation was the same as that of the compound 1a in Example 1 to obtain 36 mg of white crystals with a yield of 15%.
[0047]m.p.:174-176℃; 1 H NMR (400MHz, CDCl 3 )δ4.78–3.85(m,12H),2.64(s,9H). 13 CNMR (100MHz, CDCl 3 )δ201.42, 29.71, 20.49. HR-MS (ESI) Calcd for C 12 h 21 N 3 S 6 [M+Na]+:421.9957,found:421.9957.
Embodiment 3
[0048] The preparation of embodiment 3 compound 3a
[0049] At room temperature, take compound 1, 4, 7, 10-tetraazacyclododecane in a solvent, and prepare 327 mg of white solid with a yield of 99% according to the preparation of compound 1a in Example 1
[0050] m.p.:278-280℃ 1 H NMR (400MHz,D 2 O) δ4.70. 13 C NMR (100MHz,D 2 O) δ55.01.
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