Boc-N-甲基-L-苯丙氨酸合成路线 (共 22 条)
反应条件
2: 1.) 5N HCl, 2.) isoamyl nitrite, 3.) DIEA 3: H2 / 10percent Pd/C / ethanol; acetic acid / 760 Torr / Ambient temperature View Scheme
参考文献
Williams, Peter D.; Bock, Mark G.; Tung, Roger D.; Garsky, Victor M.; Perlow, Debra S.; et al.
Journal of Medicinal Chemistry, 1992 , vol. 35, # 21 p. 3905 - 3918
反应条件
1: 1.) 1-hydroxybenzotriazole hydrate, 1-ethyl-3-(3-(dimethylamino)propyl)carbodiimide hydrochloride / 1.) CH2Cl2, 15 min, 2.) CH2Cl2, MeOH, overnight 2: 89 percent / TFA / CH2Cl2 / 1 h 3: 1.) 1-hydroxy-7-azabenzotriazole, 1-ethyl-3-(3-(dimethylamino)propyl)carbodiimide hydrochloride, 2.) diisopropylethylamine / 1.) CH2Cl2, DMF, 15 min, 2.) CH2Cl2, DMF, overnight 4: 87 percent / TFA / CH2Cl2 / 0.17 h 5: 1.) 1-hydroxy-7-azabenzotriazole, 1-ethyl-3-(3-(dimethylamino)propyl)carbodiimide hydrochloride, 2.) diisopropylethylamine / 1.) CH2Cl2, DMF, 15 min, 2.) CH2Cl2, DMF, overnight 6: 41 percent / TFA / CH2Cl2 / 0.12 h View Scheme
参考文献
Hansen, Thomas K.; Ankersen, Michael; Hansen, Birgit S.; Raun, Kirsten; Nielsen, Karin K.; Lau, Jesper; Peschke, Bernd; Lundt, Behrend F.; Thogersen, Henning; Johansen, Nils L.; Madsen, Kjeld; Andersen, Peter H.
Journal of Medicinal Chemistry, 1998 , vol. 41, # 19 p. 3705 - 3714