双官能团伯胺-硫脲-三氟甲酸相转移催化剂催化二氢嘧啶不对称合成
symmetric Mannich-type Reaction Bifunctional Primary Amine-Thiourea-TfOH (BPAToTfOH) as Chiral Phase-Transfer Catalysts: Asymmetric Synthesis of Dihydropyrimidines
本文利用双官能团伯胺-硫脲-三氟甲酸相转移催化剂和叔丁胺三氟乙酸盐作为添加剂以饱和食盐水为溶剂在室温条件下实现了Biginelli反应的不对称合成，得到的二氢嘧啶化合物具有较高的收率和良好的对映选择性，同时对反应机理和催化剂的作用进行了讨论。
n enantioselective Biginelli reaction has been developed by using a bifunctional primary amine-thiourea-TfOH (BPAToTfOH) as a chiral phase-transfer catalyst and t-BuNH2oTFA as an additive in saturated brine at room temperature. The corresponding dihydropyrimidines were obtained in moderate-to-good yields with up to 99% ee under mild conditions. A plausible transition state has been proposed to explain the origin of the activation and the asymmetric induction.
陈茹玉、苗志伟、于吉攀、王杨云
制药化学工业有机化学工业精细化学工业
Biginelli反应手性相转移催化剂不对称合成二氢嘧啶。
Biginelli reactionChiral phase-transfer catalystAsymmetric synthesisDihydropyrimidines
陈茹玉,苗志伟,于吉攀,王杨云.双官能团伯胺-硫脲-三氟甲酸相转移催化剂催化二氢嘧啶不对称合成[EB/OL].(2011-01-11)[2025-07-17].http://www.paper.edu.cn/releasepaper/content/201101-530.点此复制
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