4-(Trifluoromethyl)benzylamine → 6-[[4-(Trifluoromethyl)phenyl]methylamino]pyridine-3-carboxamide

HRID 305

반응식

HRID 305 반응식
NC(=O)c1ccc(Cl)nc1.NCc1ccc(C(F)(F)F)cc1>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(NCc2ccc(C(F)(F)F)cc2)nc1

참가 물질

7

반응 조건

온도
100 °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 (4-(trifluoromethyl)phenyl)methanamine (0.097 mL, 0.68 mmol). The reaction was run in microwave at 100 °C for 4h. The compound was purified by preparative HPLC on a Kromasil C8 column (10 µm 250x20 ID mm) using a gradient of 51-55% acetonitrile in H2O/ACN/FA 95/5/0.2 buffer, over 25 minutes with a flow of 19 mL/min. The compounds were detected by UV at 270nm. 6-(4-(trifluoromethyl)benzylamino)nicotinamide (7.40 mg, 7.40 %) was obtained.

출처 및 근거

ORD 기록
ord-92bacb0740454b4398d7f3969518ce26
출처 데이터셋
750 AstraZeneca ELN dataset
원본 링크
출처 보기

연결된 노트

불러오는 중…