📜4-吗啉-4-基-1,2,5-三唑-3-酮置于(R,R)-(Salen)Co[oc(Cf3)3] Potassium Tert-Butylate,Potassium Iodide体系中,用 四氢呋喃 用作溶剂,化学反应 86.0H,反应生成马来酸噻吗洛尔
参考文献:Enantioselective Synthesis Of (S)-Timolol Via Kinetic Resolution Of Terminal Epoxides And Dihydroxylation Of Allylamines
标题:Enantioselective Synthesis Of (S)-Timolol Via Kinetic Resolution Of Terminal Epoxides And Dihydroxylation Of Allylamines
摘要:An Efficient Enantioselective Synthesis Of (S)-Timolol Has Been Described Using Chiral Co-Salen-Catalyzed Kinetic Resolution Of Less Expensive (+/-)-Epichlorohydrin With 3-Hydroxy-4-(N-Morpholino)-1,2,5-Thiadiazole In Good Overall Yield (55%) And Excellent Enantioselectivity (98%). Synthesis Of (S)-Timolol Has Also Been Achieved Using Hydrolytic Kinetic Resolution As Well As Asymmetric Dihydroxylation Routes In 90% Ee And 56% Ee,Respectively. (C) 2007 Elsevier Ltd. All Rights Reserved.
Doi:10.1016/j.Tet.2007.01.057