Efficient Total Synthesis of (-)-Kaitocephalin
Efficient Total Synthesis of (-)-Kaitocephalin
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DOI：
10.1021/ol9019343
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发表时间：
2009-10-15
期刊：
影响因子：
5.2
通讯作者：
Ohfune, Yasufumi
中科院分区：
文献类型：
--
作者：
Hamada, Makoto;Shinada, Tetsuro;Ohfune, Yasufumi
以5-取代脯氨酸酯为起始原料，经羟醛缩合反应、（E）-选择性α，β-脱氢氨基酸合成和催化氢化，经12步反应合成了离子型谷氨酸受体拮抗剂（-）-kaitocephalin。
A highly diastereoselective total synthesis of (-)-kaitocephalin, a novel antagonist of ionotropic glutamate receptors, was accomplished in 12 steps starting from 5-substituted proline ester via the aldol reaction with OBO-serine aldehyde, (E)-selective alpha,beta-dehydroamino acid synthesis using a new HWE reagent, and catalytic hydrogenation.