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Scalable Atroposelective Synthesis of MRTX1719 (5)

有机合成与工艺文献分享 2025-11-28 07:33
文章摘要
本文围绕MRTX1719的合成工艺展开研究。背景部分指出早期采用BocNH2与中间体21反应失败，而使用Boc2NH仅获得中等收率，且卤代酮衍生物易发生副反应。研究目的旨在开发高效稳定的合成路径，通过单锅分步构建NHBoc基团并减少分离步骤。最终采用盐酸盐23•HCl在双相体系中与Boc2O反应，利用氨水同时实现碱化、甲醛捕获和弱亲核作用，成功以定量收率获得目标产物，解决了中间体不稳定性问题。
Scalable Atroposelective Synthesis of MRTX1719 (5)
查看文献： Scalable Atroposelective Synthesis of MRTX1719: An Inhibitor of the PRMT5/MTA Complex
查看期刊：Organic Process Research & Development
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