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发明授权
CN102838621B (6R,7R)-3-甲基-7-[α-(N,N’-二异丙基脒硫基)-乙酰氨基]-8-氧代-5-硫杂-1-氮杂双环[4,2,0]-辛-2-烯-2-甲酸内铵盐晶体 有权

(6R,7R)-3-甲基-7-[α-(N,N’-二异丙基脒硫基)-乙酰氨基]-8-氧代-5-硫杂-1-氮杂双环[4,2,0]-辛-2-烯-2-甲酸内铵盐晶体
摘要：
本发明涉及(6R，7R)-3-甲基-7-[α-(N，N’-二异丙基脒硫基)-乙酰氨基]-8-氧代-5-硫杂-1-氮杂双环[4，2，0]-辛-2-烯-2-甲酸内铵盐、其晶体及其制备方法和用途。7-ADCA与溴乙酰溴反应，得到7-溴乙酰氨基-3-甲基-8-氧代-5-硫杂-1-氮杂双环[4.2.0]辛-2-烯-2-甲酸即中间体A；中间体A与N’N-二异丙基硫脲反应，得到本发明的化合物，该化合物进一步精制而制备出纯度高稳定性好的本发明化合物的晶体。本发明的化合物及其晶体对大肠杆菌、金黄色葡萄球菌、肺炎链球菌、海氏肠球菌、粪肠球菌等具有抗菌效果，尤其是对肺炎链球菌抗菌活性很强，是潜在的抗菌药物。
摘要（英）：

The invention relates to (6R,7R)-3-methyl-7-[alpha-(N,N'-diisopropyl amidine thio)-acetylamino]-8-oxo-5-thia-1-azabicyclo[4,2,0]-oct-2-alkene-2-formic betaine, crystals thereof, and preparation method and application thereof. According to the invention, 7-ADCA and bromoacetyl bromide are subjected to a reaction, such that an intermediate A, which is 7-bromo acetylamino-3-methyl-8-oxo-5-thia-1-azabicyclo [4.2.0] oct-2- alkene-2-formic acid, is obtained; the intermediate A is subjected to a reaction with N'N-diisopropyl thiourea, such that the compound provided by the invention is obtained. The compound is further refined, such that the crystals of the compound with high purity and good stability are prepared. The compound provided by the invention has antibacterial effects against escherichia coli, staphylococcus aureus, streptococcus pneumoniae, Hay enterococci, enterococcus faecalis, and the like. Especially, the compound has a high inhibiting activity against streptococcus pneumoniae. The compound is a potential antimicrobial medicine.

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