Direct catalytic asymmetric three-component Kabachnik-Fields reaction

Direct catalytic asymmetric three-component Kabachnik-Fields reaction
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DOI:
10.1002/anie.200801173
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发表时间:
2008-01-01
影响因子:
16.6
通讯作者:
List, Benjamin
List, Benjamin
中科院分区:
化学1区
文献类型:
--
作者:
Cheng, Xu;Goddard, Richard;List, Benjamin

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作为α -氨基酸的模拟物,α -氨基膦酸盐在抗菌和抗HIV药物以及蛋白酶抑制剂方面具有很大的前景。外消旋α -支化醛在新的手性磷酸催化剂1的存在下,直接与对苯胺(pmpnh2)和亚磷酸酯反应,生成具有高度非对映选择性和对映选择性的β -支化α -氨基膦酸盐。
As mimics of α‐amino acids, α‐amino phosphonates have great promise as antibacterial and anti‐HIV agents as well as protease inhibitors. Racemic α‐branched aldehydes react, in the presence the new chiral phosphoric acid catalyst 1, directly with p‐anisidine (PMPNH 2) and a phosphite to furnish β‐branched α‐amino phosphonates highly diastereoselectively and enantioselectively.