(2S,3S)-2-(3-氯苯基)-3,5,5-三甲基吗啉-2-醇合成路线 （共 6 条）
反应条件
1: (R)-(+)-1-(3-chlorophenyl)-2-hydroxypropan-1-one With trifluoromethylsulfonic anhydride; N,N,N',N'-tetra-methylnaphthalene-1,8-diamine in dichloromethane T=-50 - 0°C; 1 h; 2: 2-amino-2-methyl-propan-1-ol in dichloromethane; acetonitrile T=-10 - 0°C; 4 h;
参考文献
RESEARCH TRIANGLE INSTITUTE; CARROLL, F. Ivy; BLOUGH, Bruce E.; NAVARRO, Hernan A.; MASCARELLA, S. Wayne; MURESAN, Ana Zamfira; DAMAJ, M. Imad; LUKAS, Ronald J.
Patent: WO2011/146821 A2, 2011 ;
Location in patent: Page/Page column 54 ;
WO 2011/146821 A2
反应条件
1.1: LDA / tetrahydrofuran / -78 °C 1.2: tetrahydrofuran / -78 °C 2.1: 82 percent / AD-mix-β; H2O / 2-methyl-propan-2-ol 3.1: lutidine / CH2Cl2 / -40 °C 4.1: CH2Cl2 / -40 - 0 °C View Scheme
参考文献
Tetrahedron Asymmetry, , vol. 11, # 18 p. 3659 - 3663
反应条件
1: 82 percent / AD-mix-β; H2O / 2-methyl-propan-2-ol 2: lutidine / CH2Cl2 / -40 °C 3: CH2Cl2 / -40 - 0 °C View Scheme
参考文献
Tetrahedron Asymmetry, , vol. 11, # 18 p. 3659 - 3663
反应条件
in dichloromethane T=-40 - 0°C; cyclocondensation;
参考文献
Tetrahedron Asymmetry, , vol. 11, # 18 p. 3659 - 3663
反应条件
1: Grignard reaction; Inert atmosphere; 2: With water; ammonium chloride in tetrahydrofuran optical yield given as percent ee;
参考文献
Lukas, Ronald J.; Muresan, Ana Z.; Damaj, M. Imad; Blough, Bruce E.; Huang, Xiaodong; Navarro, Hernan A.; Mascarella, S. Wayne; Eaton, J. Brek; Marxer-Miller, Syndia K.; Carroll, F. Ivy
Journal of Medicinal Chemistry, 2010 , vol. 53, # 12 p. 4731 - 4748
反应条件
1: lutidine / CH2Cl2 / -40 °C 2: CH2Cl2 / -40 - 0 °C View Scheme
参考文献
Tetrahedron Asymmetry, , vol. 11, # 18 p. 3659 - 3663
