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A method for producing an ester-acetone write a cargo of ampicillin or amoxicillin and penicillanic acid 1,1-dioxide methane bis-diol

机译:一种生产氨苄西林或阿莫西林和青霉酸1,1-二氧化甲烷双二醇的酯-丙酮的方法

摘要

The new bis-esters (I) (R=H, OH and the imidazolidinone side chain is derived from the D-form of -amino-prenylacetic acid) and their acid addn. salts were prepd. Thus K hetacillin was esterified with iodomethyl penicillanate 1,1-dioxide to give 60% (I) (R=H). (I) are sysmetic broad spectrum antibacterial agents which can be efficiently absorbed into the gasstrointestinal tract. After absorption they are transformed into ampicillin or amoxicillin and penicillanic acid 1,1- dioxide. The latter then functions as a -lactamase inhibitor and thus increases the antibacterial activities of the ampicillin or amoxicillin.
机译:新的双酯(I)(R = H,OH和咪唑烷酮侧链衍生自-氨基-异戊烯基乙酸的D-形式)及其酸加成。制备盐。因此将Khetacillin与青霉酸碘甲基甲酯1,1-二氧化物酯化,得到60%(I)(R = H)。 (I)是可以有效吸收到胃肠道中的系统性广谱抗菌剂。吸收后,它们被转化成氨苄青霉素或阿莫西林和青霉酸1,1-二氧化物。后者然后用作-内酰胺酶抑制剂,因此增加了氨苄青霉素或阿莫西林的抗菌活性。

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