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A Fit-for-Purpose Synthesis of (R)-2-Methylazepane
Organic Process Research & Development ( IF 3.4 ) Pub Date : 2019-12-12 , DOI: 10.1021/acs.oprd.9b00425
Sylvain Guizzetti 1 , Antoine Michaut 2 , Guillaume Federspiel 1 , Julien Eymard 2 , Isabelle Caron 2 , Sabrina Quatrevaux 2 , Etienne Daras 1 , Sandrine Jolly 3 , Jérôme Guillemont 3 , David Lançois 3
Affiliation  

The preparation of new RSV inhibitors required an efficient synthesis of (R)-2-methylazepane ((R)-1) amenable to large-scale production to support preclinical studies. After consideration of different options, an efficient five-step synthesis relying on the preparation of the racemic N-Boc precursor and its purification by chiral SFC was developed and successfully implemented on a 400 g scale.

中文翻译:

目的合成(R)-2-甲基氮杂环庚烷

制备新的RSV抑制剂需要有效合成适合大规模生产的(R)-2-甲基氮杂环庚烷((R-1),以支持临床前研究。在考虑了不同的选择之后,开发了一种有效的五步合成方法,该方法依赖于外消旋N- Boc前体的制备及其通过手性SFC的纯化,并成功实现了400 g的规模。
更新日期:2019-12-12
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