Fmoc-L-天门冬氨酸4-叔丁酯合成路线 （共 32 条）
反应条件
1: fmoc-O-tert-butyl-L-tyrosine With benzotriazol-1-ol; N-ethyl-N,N-diisopropylamine; diisopropyl-carbodiimide in N,N-dimethyl-formamide 1 h; 2: With piperidine in N,N-dimethyl-formamide 0.5 h; 3: N-(fluoren-9-ylmethoxycarbonyl)-L-Val; N-(9-fluorenylmethoxycarbonyl)-L-aspartic acid-β-(tert-butyl)ester; N-(fluoren-9-ylmethoxycarbonyl)-L-Lys(Nε-Boc); N-α-Fmoc-N-ω,N-ω'-bis-tert-butoxycarbonyl-L-arginine Further stages;
参考文献
Organic Process Research and Development, , vol. 14, # 6 p. 1313 - 1325
反应条件
triethylsilane; water; trifluoroacetic acid 0.5 h;
参考文献
Palladino, Pasquale; Stetsenko, Dmitry A.
Organic Letters, 2012 , vol. 14, # 24 p. 6346 - 6349
反应条件
triethylsilane; water; trifluoroacetic acid 0.5 h;
参考文献
Journal of Peptide Science, , vol. 16, # 3 p. 159 - 164
反应条件
1: N-(9-fluorenylmethoxycarbonyl)-L-aspartic acid-β-(tert-butyl)ester With N-ethyl-N,N-diisopropylamine in methanol; dichloromethane 1.25 h; 2: With piperidine; 1,8-diazabicyclo[5.4.0]undec-7-ene in N,N-dimethyl-formamide 0.25 h; 3: acetic anhydride Further stages;
参考文献
ASCENDIS PHARMA OPHTHALMOLOGY DIVISION A/S; RAU, Harald; KNAPPE, Thomas; LAUFER, Burkhardt; REIMANN, Romy; WEISBROD, Samuel; SPROGØE, Kennett; BISEK, Nicola; STARK, Sebastian; VOIGT, Tobias
Patent: WO2014/56923 A1, 2014 ;
Location in patent: Page/Page column 146; 147 ;
反应条件
1: N,N'-dicyclohexylcarbodiimide / tetrahydrofuran 2: CF3CO2H / CH2Cl2 / 0.5 h View Scheme
参考文献
Lee, Dennis; Adams, Jerry L.; Brandt, Martin; DeWolf Jr., Walter E.; Keller, Paul M.; Levy, Mark A.
Bioorganic and Medicinal Chemistry Letters, 1999 , vol. 9, # 12 p. 1667 - 1672
反应条件
1: With 4-methyl-morpholine in ethylene glycol dimethyl ether T=-15°C; 1 h; 2: With sodium tetrahydroborate in ethylene glycol dimethyl ether; water T=-15°C; Further stages.;
参考文献
Boeijen; Van Ameijde; Liskamp
Journal of Organic Chemistry, 2001 , vol. 66, # 25 p. 8454 - 8462
反应条件
sodium borohydride in tetrahydrofuran; methanol; ammonium chloride
参考文献
Merck Frosst Canada and Co.
Patent: US6552168 B1, 2003 ;
US 6552168 B1
反应条件
pyridine; di-tert-butyl dicarbonate; ammonium hydrogen carbonate T=20°C;
参考文献
Chu, Chi-Yuan; Chang, Chun-Ping; Chou, Yun-Ting; Handoko; Hu, Yi-Ling; Lo, Lee-Chiang; Lin, Jing-Jer
Journal of Medicinal Chemistry, 2013 , vol. 56, # 7 p. 2841 - 2849
反应条件
Yield given. Multistep reaction;
参考文献
Schnorrenberg; Gerhardt
Tetrahedron, 1989 , vol. 45, # 24 p. 7759 - 7764
反应条件
1: Pd(PPh3)4; PhSiH3
2: TFA; triisopropylsilane; water / 2 h
View Scheme
参考文献
Boturyn, Didier; Dumy, Pascal
Tetrahedron Letters, 2001 , vol. 42, # 15 p. 2787 - 2790
