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| 摘要: |
| 目的 研究头孢硫脒的合成工艺，使之适合工业化生产，并提高收率。方法 以7-ACA为原料，与溴乙酰溴在低温、碱性条件下经C-7位上的氨基酰化，再同侧链二异丙基硫脲缩合制得头孢硫脒。结果 总收率由45%提高到62%，产物经IR，MS，1H-NMR确证结构。结论 改进后的工艺过程大为简化，总收率得到了提高，适合于工业化生产。 |
| 关键词: 头孢硫脒 头孢菌素 合成 |
| DOI： |
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| Improved Synthesis Process of Cefathiamidine |
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WANG Honglin LI Liwei*
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| Abstract: |
| OBJECTIVE To synthesize the title compound and improve process to make it suitable for industrial production, and increase yield. METHODS Cefathiamidine was synthesized from 7-ACA as starting material, acylated by bromoacetyl bromide at C-7 position in a low temperature and alkaline condition, and then condensed by side chain diisopropylthiourea. RESULTS The overall yield was increased from 45% to 62%, the structure of product was confirmed by IR, MS, and 1H-NMR. CONCLUSION The improved process was greatly simplified, with a total yield improved, and suitable for industrial production. |
| Key words: cefathiamidine cephalosporin synthesis |
