Synthesis method of nami- serte, an oral pulmonary fibrosis drug
CN122917049APending Publication Date: 2026-10-16HANGZHOU CHEMINSPIRE TECH CO LTD
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Patent Information
- Application Number
- CN202611251819.4
- Authority / Receiving Office
- CN · China
- Patent Type
- Applications(China)
- Current Assignee / Owner
- Filing Date
- 2026-08-18
- Publication Date
- 2026-10-16
AI Technical Summary
Benefits of technology
[0033]本发明关于那米司特的合成方法，优化了离去基团引入关键乙酰基中间体化合物6并将其用于合成那米司特N1乙酰中间体化合物10，改进了缩合反应减少了合成步骤，优化了手性膦配体催化的手性亚砜的合成，并利用乙酰基保护基团提高了N1中间体的结晶性能使中间体的光学纯度进一步得到提高，利于提高最终成品纯度。路线总收率也得到了提高，极大提高了合成效率，极大降低了工艺成本。该路线操作简单，不仅总收率较高，得到的产品纯度也较高，适合放大生产。
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Abstract
The application provides a synthesis method of namilumide. Compound 1 is used as a starting material, and a key acetyl chiral sulfoxide compound 6 is synthesized through two methods: one-pot cyclization of compound 7 and (2-chloro-3-dimethylamino-2-propenyl)dimethylammonium salt to obtain compound 8, and then removing the amino protection to obtain compound 9; finally, efficient condensation of compound 6 and compound 9 obtains compound 10, and then removing the acetyl protection group to obtain the target product namilumide compound 11. The synthesis route is short, simple in operation, high in yield and selectivity, and suitable for the synthesis method of namilumide for industrial production. The route is as follows:
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