Development of a General Protocol To Prepare 2&ITH&IT-1,3-Benzoxazine Derivatives
Development of a General Protocol To Prepare 2&ITH&IT-1,3-Benzoxazine Derivatives
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DOI：
10.1021/acs.oprd.7b00209
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发表时间：
2017-10-01
影响因子：
3.4
通讯作者：
Brands, Karel M. J.
中科院分区：
文献类型：
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作者：
Qi, Ji;Oliver, Steven F.;Brands, Karel M. J.
介绍了醛胺和三氟甲烷磺酸催化合成2h -1,3-苯并恶嗪衍生物的实际合成和详细开发过程。探索了具有不同空间和电子性质的广泛衬底。脂肪族/芳香族/杂芳香族底物在优化成稳健、可扩展工艺的条件下都进行得很好。
A practical synthesis and detailed development process of 2H-1,3-benzoxazine derivatives catalyzed by aldimine and trifluoromethanesulfonic acid is described. A broad range of substrates with diverse steric and electronic properties were explored. Aliphatic/aromatic/heteroaromatic substrates all proceed well under conditions which have been optimized into a robust, scalable process.