New learning discoveries about 675109-45-2

Reference of 675109-45-2, These common heterocyclic compound, 675109-45-2, name is 6-Amino-2,3-dihydro-1H-isoindol-1-one, 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.

Reference of 675109-45-2, These common heterocyclic compound, 675109-45-2, name is 6-Amino-2,3-dihydro-1H-isoindol-1-one, 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.

To a solution of 6-aminoisoindolin-1-one (0.675 mmol) in 1,2-dichloroethane (0.2 M) was added 2,6-dichloro-4-fluorobenzaldehyde (0.675 mmol), NaBH(OAc)3 (2.025 mmol), and acetic acid (0.675 mmol, 39tL). The mixture was stirred at 80 C for 24 hours. The reaction mixture was quenched with sat.NaHCO3 and extracted with EtOAc. The organic layer was then washed with water and brine, dried over Na2SO4, filtered and evaporated. The crude was purified by preparative HPLC to give the desired compound 300 (Yield = 21%, white cotton). ?H NIVIR (400 1VIHz, DMSO) 8.36 (s, 1H), 7.61 (d, J= 8.6 Hz, 2H), 7.28 (d, J= 8.1 Hz, 1H), 7.05 – 6.82 (m, 2H), 6.02 (t, J 4.9 Hz,1H), 4.40 (d, J= 4.9 Hz, 2H), 4.21 (s, 2H). ?3C NIVIR (101 1VIHz, DMSO) 170.99 (s), 148.98 (s),136.86 (s), 136.74 (s), 133.95 (s), 132.17 (s), 131.24 (s), 124.22 (s), 117.36 (s), 116.88 (s), 116.63 (s), 104.66 (s), 44.75 (s), 43.23 (s).

Statistics shows that 6-Amino-2,3-dihydro-1H-isoindol-1-one is playing an increasingly important role. we look forward to future research findings about 675109-45-2.

Reference:
Patent; THE CENTRE FOR DRUG RESEARCH AND DEVELOPMENT; THE UNIVERSITY OF BRITISH COLUMBIA; ROBERGE, Michel; BARADARAN-HERAVI, Alireza; BALGI, Aruna D.; ZIMMERMANN, Carla D.; KRAUSE, Alexandra; PFEIFER, Thomas Arthur; JAQUITH, James Brian; TAN, Jason Samuel; SHIDMOOSSAVEE, Fahimeh S.; ARNS, Stephen Paul; BAUDELET, Davy Jeremy; (354 pag.)WO2017/49409; (2017); A1;,
Indoline – Wikipedia,
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