A common heterocyclic compound, 222036-66-0, name is 5-Aminoisoindolin-1-one, molecular formula is C8H8N2O, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route. 222036-66-0.
Intermediate 8 (50 mg, 0.162 mmol), 5-amino-2,3-dihydro-isoindol-l-one (72 mg, 0.485 mmol), glacial acetic acid (9 mul, 0.162 mmol) and n-butanol (1.5 ml) were combined and irradiated at 150 0C for 60 minutes in a Biotage 1-60 microwave reactor. The reaction was evaporated, purified by LCMS (low pH buffer) triturated with methanol and dried to give the title compound as a white solid (6 mg, 7percent). 1H NMR (400 MHz, DMSOd6) delta ppm 0.55 – 0.61 (m, 2 H), 0.87 – 0.93 (m, 2 H), 1.50 – 1.57 (m, 1 H), 1.64 – 1.77 (m, 3 H), 1.78 – 1.90 (m, 1 H), 1.91 – 2.00 (m, 2 H), 2.02 – 2.13 (m,2 H), 2.88 – 2.98 (m, 1 H), 3.09 – 3.16 (m, 2 H), 3.28 – 3.56 (m, 2 H), 4.38 (s, 2 H), 7.61 – 7.69 (m,3 H), 7.71 – 7.77 (m, 1 H), 7.86 – 7.91 (m, 1 H), 8.37 – 8.53 (m, 2 H), 10.39 (br. s, 1 H); m/z (ES+APCI)+: 421 [M+H]+.
The synthetic route of 5-Aminoisoindolin-1-one has been constantly updated, and we look forward to future research findings.
Reference:
Patent; MEDICAL RESEARCH COUNCIL; WO2009/122180; (2009); A1;,
Indoline – Wikipedia,
Indoline | C8H9N – PubChem