An efficient and cost-effective synthesis of 2-phenyl-3-aminopyridine
An efficient and cost-effective synthesis of 2-phenyl-3-aminopyridine
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DOI：
10.1021/op000227e
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发表时间：
2001-05-01
影响因子：
3.4
通讯作者：
Braish, TF
中科院分区：
文献类型：
--
作者：
Caron, S;Massett, SS;Braish, TF
以2-氯-3-氨基吡啶为原料，用亚胺作氨基吡啶的保护基，合成了2-苯基-3-氨基吡啶，它是制备2-苯基-3-氨基哌啶的关键中间体。2-氯-3-氨基吡啶用苯甲醛原位保护，然后与苯基硼酸进行Suzuki偶联，再经酸水解，从廉价和可商购的起始材料的高产率步骤。
The synthesis of 2-phenyl-3-aminopyridine, a key intermediate in the preparation of 2-phenyl-3-aminopiperidine, from 2-chloro-3-aminopyridine is described using an imine as a protecting group for an aminopyridine, The in situ protection of 2-chloro-3-aminopyridine with benzaldehyde followed by Suzuki coupling with phenylboronic acid and subsequent acid hydrolysis provided the titled compound in a single, high-yielding step from inexpensive and commercially available starting materials.