106429-59-8, name is 2-Oxo-2,3-dihydro-1H-benzo[d]imidazole-5-carbaldehyde, belongs to imidazoles-derivatives compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. name: 2-Oxo-2,3-dihydro-1H-benzo[d]imidazole-5-carbaldehyde
Step 3. N-(2-amino-2-oxoethyl)-N-(5-fluoro-2-((4-(7-((2-oxo-2,3-dihydro-1H- benzo[d]imidazol-5-yl)methyl)-2,7-diazaspiro[4.4]nonan-2-yl)pyrimidin-5- yl)oxy)phenyl)isobutyramide (1176) To a solution of N-(2-((4-(2,7-diazaspiro[4.4]nonan-2-yl)pyrimidin-5-yl)oxy)-5- fluorophenyl)-N-(2-amino-2-oxoethyl)isobutyramide (40 mg, crude) and 2-oxo-2,3- dihydro-1H-benzo[d]imidazole-5-carbaldehyde (Intermediate 40, 29 mg, 0.18 mmol) in anhydrous MeOH (4 mL) was added 4A-molecular sieves (50 mg), then the reaction was stirred at 50 C for 2 h under N2. After 2 h, NaBH3CN (28 mg, 0.45 mmol) was added into the solution and the reaction mixture was stirred at 50 C for 12 h. The reaction mixture was then filtered, concentrated under reduced pressure, and purified by RP- HPLC method G to afford N-(2-amino-2-oxoethyl)-N-(5-fluoro-2-((4-(7-((2-oxo-2,3- dihydro-1H-benzo[d]imidazol-5-yl)methyl)-2,7-diazaspiro[4.4]nonan-2-yl)pyrimidin-5- yl)oxy)phenyl)isobutyramide as a white solid.Yield: 7.00 mg. LCMS method E: Rt = 1.498 min, (M+H)+ = 603.3.1H NMR (CD3OD): delta 8.30 (s, 1 H), 7.76 (d, J = 2.4 Hz, 1 H), 7.52 (d, J = 8.8 Hz, 1 H), 7.15 (t, J = 8.0 Hz, 1 H), 6.87-7.03 (m, 4 H), 4.73 (dd, J = 16.4, 3.6 Hz, 1 H), 3.82 (dd, J =16.0, 4.8 Hz, 1 H), 3.56-3.85 (m, 5 H), 2.45-2.69 (m, 5 H), 1.81-1.94 (m, 5 H), 1.05 (dd, J = 36.8, 6.8 Hz, 6 H).19F NMR (CD3OD): delta -119.24.
The synthetic route of 106429-59-8 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; VITAE PHARMACEUTICALS, INC.; CACATIAN, Salvacion; CLAREMON, David, A.; DILLARD, Lawrence, Wayne; DONG, Chengguo; FAN, Yi; JIA, Lanqi; LOTESTA, Stephen, D.; MARCUS, Andrew; MORALES-RAMOS, Angel; SINGH, Suresh, B.; VENKATRAMAN, Shankar; YUAN, Jing; ZHENG, Yajun; ZHUANG, Linghang; PARENT, Stephan, D.; HOUSTON, Travis, L.; (444 pag.)WO2017/214367; (2017); A1;,
Imidazole – Wikipedia,
Imidazole | C3H4N2 – PubChem