496-12-8, The chemical industry reduces the impact on the environment during synthesis 496-12-8, name is Isoindoline, I believe this compound will play a more active role in future production and life.
Isoindoline (20 mu, 0.18 mmol) was added to a stirred suspension of3- (2-(4-fluorophenyl)-3-(methylcarbamoyl)benzofuran-5-yl)benzoic acid (20 mg, 0.051 mmol), HATU (25 mg, 0.066 mmol), and DIPEA (50 mu, 0.29 mmol) in DMF (0.5 mL). The reaction was stirred at r.t. overnight. The reaction was then diluted with MeOH and an off-white ppt. formed. The ppt. was collected by filtration, triturated with MeOH, and air dried to afford the title compound (17 mg, 68% yield). ? NMR (500 MHz, DMSO-i?) delta ppm 8.50 (q, J= 4.58 Hz, 1 H) 7.99 – 8.05 (m, 2 H) 7.90 – 7.95 (m, 2 H) 7.85 (dt, J= 6.10, 2.44 Hz, 1 H) 7.77 – 7.81 (m, 1 H) 7.73 – 7.77 (m, 1 H) 7.58 – 7.64 (m, 2 H) 7.36 – 7.45 (m, 3 H) 7.30 – 7.34 (m, 1 H) 7.29 (s, 2 H) 4.91 (s, 2 H) 4.84 (s, 2 H) 2.86 (d, J = 4.88 Hz, 3 H). LC/MS was performed on a Shimadzu-VP instrument with UV detection at 220 nm and Waters Micromass. LC/MS method: solvent A = 10% CH3CN/90% H2O/0.1% TFA, solvent B = 90% CH3CN/10% H2O/0.1% TFA, start %B = 0, final %B = 100, gradient time = 3 min, stop time = 4 min, flow rate = 4 ml/min, column: Sunfire CI 8 5 muiotaeta 4.6 x 50 mm; HPLC Rt = 2.48 min, (ES+) m/z (MH+) = 491. Analytical HPLC method: solvent A = 5% CH3CN/95% H2O/0.1% TFA, solvent B = 95% CH3CN/5% H2O/0.1% TFA, start %B = 10, final %B = 100, gradient time = 15 min, stop time = 18 min, flow rate = 1 ml/min. Column: Waters Sunfire C-18, 3.5 muiotaeta 4.6 x 150 mm, Rt = 13.81 min, purity = 100%; column: Waters Xbridge Phenyl 3.5 muiotaeta 4.6 x 150 mm, Rt = 13.81 min, purity = 100%.
The chemical industry reduces the impact on the environment during synthesis Isoindoline. I believe this compound will play a more active role in future production and life.
Reference:
Patent; BRISTOL-MYERS SQUIBB COMPANY; YEUNG, Kap-Sun; PARCELLA, Kyle, E.; BENDER, John, A.; BENO, Brett, R.; GRANT-YOUNG, Katharine, A.; HAN, Ying; HEWAWASAM, Piyasena; KADOW, John, F.; NICKEL, Andrew; WO2011/112191; (2011); A1;,
Indoline – Wikipedia,
Indoline | C8H9N – PubChem