Tert-butyl 3-(2-aminoacetamido)azetidine-1-carboxylate → Tert-butyl 3-(2-((2,6-bis(trifluoromethyl)quinazolin-4-yl)amino)acetamido)azetidine-1-carboxylate
反応式
Cl[C:2]1[C:11]2[C:6](=[CH:7][CH:8]=[C:9]([C:12]([F:15])([F:14])[F:13])[CH:10]=2)[N:5]=[C:4]([C:16]([F:19])([F:18])[F:17])[N:3]=1.[NH2:20][CH2:21][C:22]([NH:24][CH:25]1[CH2:28][N:27]([C:29]([O:31][C:32]([CH3:35])([CH3:34])[CH3:33])=[O:30])[CH2:26]1)=[O:23]>C1COCC1>[F:17][C:16]([F:19])([F:18])[C:4]1[N:3]=[C:2]([NH:20][CH2:21][C:22]([NH:24][CH:25]2[CH2:28][N:27]([C:29]([O:31][C:32]([CH3:35])([CH3:34])[CH3:33])=[O:30])[CH2:26]2)=[O:23])[C:11]2[C:6](=[CH:7][CH:8]=[C:9]([C:12]([F:15])([F:14])[F:13])[CH:10]=2)[N:5]=1参加物
4
実験手順
A mixture of 4-chloro-2,6-bis(trifluoromethyl)quinazoline (120 mg, 0.399 mmol, prepared in the previous step), tert-butyl 3-(2-aminoacetamido)azetidine-1-carboxylate (133 mg, 0.58 mmol, prepared in Example 1, Step E) and TEA (0.12 mL, 0.863 mmol) was dissolved in dry THF (10 mL) and heated to reflux under argon for 18 hours. The reaction mixture as concentrated in vacuo and the residue purified by flash chromatography (silica gel, 50% EtOAc/Heptane).