Reference of 675109-45-2, In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 675109-45-2, name is 6-Amino-2,3-dihydro-1H-isoindol-1-one belongs to indolines-derivatives compound, it is a common compound, a new synthetic route is introduced below.
6-Ammnoisoindolin-1-one (15.34 mg, 0.104 mmol) was dissolved in DCM (1.0 mL) along with pyridine (0.039 mL, 0.487 mmol) and DIEA (0.032 mL, 0.183 mmol). Intermediate 14SF (28 mg, 0.061 mmol) in 2 mL of DCM was added dropwise, and the reaction mixture was stirred at room temperature for 50 minutes. The reaction was quenched with 1.0 N HC1 (0.5 mL). All solvent was removed under vacuum. The crudewas dissolved in DMSO/THF (2:1, 6 mL) and purified via preparative LC/MS (method C,40-100% B over 18 mm, then a 5-mm hold at 100% B). Fractions containing the desired product were combined and dried via centrifugal evaporation to yield Example 178 (10.7 mg, 31% yield). ?H NMR (500MHz, DMSO-d6) 8.72 (s, 1H), 8.56 (s, 1H), 8.51 (br. s., 1H), 7.86 (d, J=10.7 Hz, 2H), 7.81 (br. s., 2H), 7.61 (br. s., 1H), 7.46 (d, J=5.8 Hz, 1H),5.48-5.38 (m, 1H), 4.54 (d, J12.2 Hz, 1H), 4.41 (dd, J=12. 1, 7.2 Hz, 1H), 4.29 (s, 2H),4.08 (s, 3H), 3.64 (dd, J15.9, 9.8 Hz, 1H), 3.36 (d, J=13.7 Hz, 1H), 2.62 (s, 3H);LC-MS: method C, 2 to 98% B. RT = 2.21 mm, MS (ESI) m/z: 572.30 (M+H).Analytical HPLC purity (method B): 100%.
The synthetic route of 6-Amino-2,3-dihydro-1H-isoindol-1-one has been constantly updated, and we look forward to future research findings.
Reference:
Patent; BRISTOL-MYERS SQUIBB COMPANY; ZHANG, Xiaojun; PRIESTLEY, Eldon Scott; HALPERN, Oz Scott; JIANG, Wen; REZNIK, Samuel Kaye; RICHTER, Jeremy M.; (545 pag.)WO2018/13776; (2018); A1;,
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