2-(Trifluoromethyl)benzylamine → 6-[[2-(Trifluoromethyl)phenyl]methylamino]pyridine-3-carboxamide

HRID 303

반응식

HRID 303 반응식
NC(=O)c1ccc(Cl)nc1.NCc1ccccc1C(F)(F)F>CC(=O)O.CC(=O)O.CC(C)(C)[O-].COCCOC.[Na+].[Pd].c1ccc(P(c2ccccc2)c2ccc3ccccc3c2-c2c(P(c3ccccc3)c3ccccc3)ccc3ccccc23)cc1>NC(=O)c1ccc(NCc2ccccc2C(F)(F)F)nc1

참가 물질

7

반응 조건

온도
120 °C

실험 절차

To a stirred solution of 6-chloronicotinamide (0.053 g, 0.34 mmol), 2,2'-bis(diphenylphosphino)-1,1'-binaphthyl (0.021 g, 0.03 mmol), sodium 2-methylpropan-2-olate (0.065 g, 0.68 mmol) and diacetoxypalladium (7.60 mg, 0.03 mmol) in DME (1 mL) was added (2-(trifluoromethyl)phenyl)methanamine (0.095 mL, 0.68 mmol). The reaction mixture was subjected to microwave irradiation for 4h at 120 C. Only traces of product was observed. The crude product was dissolved in DMSO (2 mL) and purified using Fractionlynx I, (Xbridge Prep C18 5µm OBD 19x150 mm column), with 5 to 95% acetonitrile in 0.2% ammonia at pH 10. 6-(2-(trifluoromethyl)benzylamino)nicotinamide: 1.45 mg (1.5 %)

출처 및 근거

ORD 기록
ord-c7ac817750064edba47d3c6c786a7b69
출처 데이터셋
750 AstraZeneca ELN dataset
원본 링크
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