(2S,3R)-3-(Boc-氨基)-2-羟基-4-苯基丁酸合成路线 （共 25 条）
反应条件
1: methanol / 2 h / 20 °C 2: TEMPO; NaClO2; NaClO / aq. phosphate buffer; acetonitrile / 35 °C / pH 6.7 View Scheme
参考文献
Tetrahedron Asymmetry, , vol. 13, # 11 p. 1201 - 1208
反应条件
1: With borane-THF in tetrahydrofuran T=0 - 20°C; 16 h; 2: With water in tetrahydrofuran T=0 - 12°C; 0.333333 h;
参考文献
G. D. Searle and Co.
Patent: US6388132 B1, 2002 ;
Location in patent: Page column 43 ;
反应条件
1: 87 percent / EDAC; HOBt; DIPEA / dimethylformamide; CH2Cl2 / 12 h / 20 °C 2: 95 percent / hydrogen / Pd/C / methanol / 3 h / 20 °C 3: 85 percent / TFA / CH2Cl2 / 12 h / 20 °C View Scheme
参考文献
Righi, Giuliana; D'Achille, Claudia; Pescatore, Giovanna; Bonini, Carlo
Tetrahedron Letters, 2003 , vol. 44, # 37 p. 6999 - 7002
反应条件
1: Fmoc-Leu-Wang resin With piperidine in N,N-dimethyl-formamide 0.5 h; solid phase reaction; 2: N-Boc-(2S,3R)-3-amino-2-hydroxy-4-phenylbutyric acid With N-ethyl-N,N-diisopropylamine; HATU in N,N-dimethyl-formamide 1 h; solid phase reaction; 3: With tri-iso-propylsilane; trifluoroacetic acid in tetrahydrofuran; water; N,N-dimethyl-formamide 2 h; solid phase reaction;
参考文献
Velmourougane, Geetha; Harbut, Michael B.; Dalal, Seema; McGowan, Sheena; Oellig, Christine A.; Meinhardt, Nataline; Whisstock, James C.; Klemba, Michael; Greenbaum, Doron C.
Journal of Medicinal Chemistry, 2011 , vol. 54, # 6 p. 1655 - 1666
反应条件
1: N-Fmoc-L-leucine With 4-(N,N-dimethlyamino)pyridine; Paramax Wang resin; N-ethyl-N,N-diisopropylamine; HATU 1 h; solid phase reaction; 2: With piperidine; 1,8-diazabicyclo[5.4.0]undec-7-ene in N,N-dimethyl-formamide 0.5 h; solid phase reaction; 3: N-Boc-(2S,3R)-3-amino-2-hydroxy-4-phenylbutyric acid Further stages;
参考文献
Velmourougane, Geetha; Harbut, Michael B.; Dalal, Seema; McGowan, Sheena; Oellig, Christine A.; Meinhardt, Nataline; Whisstock, James C.; Klemba, Michael; Greenbaum, Doron C.
Journal of Medicinal Chemistry, 2011 , vol. 54, # 6 p. 1655 - 1666
