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A mixture of 6-(trifluoromethoxy)indoline [CAS 959235-95-1 ] (837 mg, 4.12 mmol), 2-(2-(2-((fe/t-butyldimethylsilyl)oxy)ethoxy)-4-chlorophenyl)-2-((3-methoxy-5-(1 /-/- 1 ,2,4-triazol-1 -yl)phenyl)amino)acetic acid 5d (2.196 g, 4.12 mmol), HATU (2.35 g, 6.18 mmol) and diisopropylethylamine (2 ml_, 12.36 mmol) in DMF (20 ml_) was stirred at room temperature for 2 h. The mixture was diluted with water. The resulting gummy material was taken up with EtOAc, washed with a solution of K2CO3 10% in water, water, dried over MgSO4, filtered and the solvent was concentrated under reduced pressure. The residue was purified by flashchromatography on silica gel (15-40 muiotatauiota, 80 g, heptane/EtOAc gradient 70/30 to 60/40). The pure fractions were combined and the solvent was concentrated under reduced pressure to give 2-(2-(2-((terf-butyldimethylsilyl)oxy)ethoxy)-4- chlorophenyl)-2-((3-methoxy-5-(1 H-1 ,2,4-triazol-1 -yl)phenyl)amino)-1 -(6- (trifluoromethoxy)indolin-1 -yl)ethanone 6a (1 .65 g).
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Reference:
Patent; JANSSEN PHARMACEUTICALS, INC.; KATHOLIEKE UNIVERSITEIT LEUVEN; KESTELEYN, Bart Rudolf Romanie; BONFANTI, Jean-Francois; COESEMANS, Erwin; RABOISSON, Pierre Jean-Marie Bernard; MARCHAND, Arnaud Didier M; BARDIOT, Dorothee Alice Marie-Eve; (92 pag.)WO2018/178240; (2018); A1;,
Indoline – Wikipedia,
Indoline | C8H9N – PubChem