(1S,3aR,6aS)-2-[(2S)-2-[[(2S)-2-环己基-2-[(2-吡嗪基羰基)氨基]乙酰基]氨基]-3,3-二甲基-1-氧代丁基]八氢环戊并[c]吡咯-1-羧酸叔丁酯合成路线 (共 3 条)
反应条件
hydrogenchloride; water in formic acid T=0°C; 3.3 h; Product distribution / selectivity;
参考文献
Tanoury, Gerald J.; Chen, Minzhang; Cochran, John E.
Patent: US2007/87973 A1, 2007 ;
Location in patent: Page/Page column 21; 48-49 ;
反应条件
1-propanephosphonic acid cyclic anhydride; N-ethyl-N,N-diisopropylamine in ethyl acetate
T=0 - 20°C; 25 h; Overall yield = 43 percent; Overall yield = 27 mg;
参考文献
SANDOZ AG; FELZMANN, Wolfgang; BRUNNER, Stefanie; WILHELM, Thorsten
Patent: WO2013/135870 A1, 2013 ;
Location in patent: Page/Page column 19-20 ;
反应条件
1: 2-carboxypyrazine With 1,1'-carbonyldiimidazole in N,N-dimethyl-formamide
T=20 - 30°C; 1.5 h;
2: (1S,3aR,6aS)-tert-butyl 2-((S)-2-((S)-2-amino-2-cyclohexylacetamido)-3,3-dimethylbutanoyl)octahydrocyclopenta[c]pyrrole-1-carboxylate in N,N-dimethyl-formamide
T=15 - 30°C; 1 h;
3: With potassium carbonate in water; N,N-dimethyl-formamide
T=0°C; Product distribution / selectivity;
参考文献
Tanoury, Gerald J.; Chen, Minzhang; Cochran, John E.
Patent: US2007/87973 A1, 2007 ;
Location in patent: Page/Page column 21; 47-48 ;