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发明公开
CN104262359A 一种舒巴坦酸的合成方法 有权 质押

一种舒巴坦酸的合成方法
摘要：
本发明公开了一种舒巴坦酸的合成方法，包括将6-氨基青霉烷酸经重氮化溴化反应形成双溴代青霉素烷酸，然后经过氧化反应、还原反应得到舒巴坦酸；所述重氮化溴化反应中，6-氨基青霉烷酸采用酸溶液的形式连续加入，所述6-氨基青霉烷酸的酸溶液为5％～8％的硫酸水溶液、13％～15％的氢溴酸水溶液或5％～8％的盐酸水溶液。本发明采用酸溶液的方式滴加6-氨基青霉烷酸，避免了粉尘污染，提高了现场人员的工作环境；同时保证6-氨基青霉烷酸以稳定的盐的形式存在，避免发生分解反应，提高了反应质量，采用本发明的方法三步收率70％以上，HPLC纯度99.7％以上，单杂
摘要（英）：

The invention discloses a synthetic method of salbactam acid. The synthetic method comprises the following steps: carrying out diazotized bromination reaction on 6-aminopenicillanic acid to form bromopenicillanic acid; and then, carrying out oxidation reaction and reduction reaction to obtain salbactam acid, wherein in the diazotized bromination reaction, 6-aminopenicillanic acid is continuously added in form of an acidic solution, the acidic solution of 6-aminopenicillanic acid is 5-8% sulfuric acid aqueous solution, 13-15% hydrobromic acid aqueous solution or 5-8% hydrochloric acid aqueous solution. 6-aminopenicillanic acid is dropwise added in form of the acidic solution, so that dust pollution is avoided and the work environment of field personnel is improved. Meanwhile, 6-aminopenicillanic acid exists in form of stable salt, decomposition reaction is avoided, and the reaction quality is improved. The three-step yield of the method is over 70%, the HPCL purity is over 99.7%, the individual impurity content is less than 0.1% and the total impurity content is less than 0.5%.

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