Each compound has different characteristics, and only by selecting the characteristics of the compound suitable for a specific situation can the compound be applied on a large scale. 959235-95-1, name is 6-(Trifluoromethoxy)indoline, This compound has unique chemical properties. The synthetic route is as follows., Safety of 6-(Trifluoromethoxy)indoline
HATU (1 .54 g, 4.06 mmol) was added to a mixture of 6-(trifluoromethoxy)indoline [CAS 953906-76-8] (550 mg, 2.70 mmol), 2-(4-chloro-2-fluorophenyl)-2-((3- (2-hydroxyethoxy)-5-methoxyphenyl)amino)acetic acid 2e (1 g, 2.70 mmol) and diisopropylethylannine (1 .34 mL, 8.1 1 mmol) in DMF (30 mL). The resulting mixture was stirred at room temperature for 12 h. The mixture was diluted with water. The precipitate was filtered off, and washed with water. The solid was dissolved in EtOAc, washed with a 10% solution of K2CO3 in water and then with brine. The organic layer was dried over MgSO4, filtered, and the solvent was evaporated under reduced pressure. The crude residue was purified by flash chromatography on silica gel (15-40 muetaeta, 80 g, CH2CI2/MeOH 99.5/0.5) to afford 2-(4-chloro-2-fluorophenyl)-2-((3-(2-hydroxyethoxy)-5-methoxyphenyl)amino)-1 -(6-(trifluoro- methoxy)indolin-1 -yl)ethanone (Compound 6, 500 mg). An analytical sample of Compound 6 was obtained by crystallized from diisopropyl ether. Compound 6: 1H NMR (500 MHz, DMSO-cfe) delta ppm 3.14 – 3.22 (m, 2 H) 3.58 – 3.68 (m, 5 H) 3.80 – 3.90 (m, 2 H) 4.05 – 4.15 (m, 1 H) 4.38 – 4.47 (m, 1 H) 4.80 (t, J=5.5 Hz, 1 H) 5.70 (d, J=9.1 Hz, 1 H) 5.79 (t, J=1 .9 Hz, 1 H) 5.93 (d, J=1 .9 Hz, 2 H) 6.63 (d, J=9.1 Hz, 1 H) 7.03 (dd, J=8.2, 1 .6 Hz, 1 H) 7.31 – 7.37 (m, 2 H) 7.42 – 7.51 (m, 2 H) 8.02 (s, 1 H) LC/MS (method LC-A): Rt 3.39 min, MH+ 555 Melting point: 166C
Chemical properties determine the actual use. Each compound has specific chemical properties and uses. We look forward to more synthetic routes in the future to expand reaction routes of 959235-95-1.
Reference:
Patent; JANSSEN PHARMACEUTICALS, INC.; KATHOLIEKE UNIVERSITEIT LEUVEN; BARDIOT, Dorothee Alice Marie-Eve; BONFANTI, Jean-Francois; KESTELEYN, Bart Rudolf Romanie; MARCHAND, Arnaud Didier M; RABOISSON, Pierre Jean-Marie Bernard; (76 pag.)WO2017/167953; (2017); A1;,
Indoline – Wikipedia,
Indoline | C8H9N – PubChem