3-Fluoro-N-trifluoroacetylbenzylamine → HCID 178431089, 화합물

온도

50 °C

Following general procedure F using 2,2,2‐trifluoro‐N‐(3‐fluorobenzyl)acetamide (55.3 mg, 0.25 mmol), B2pin2 (127 mg, 0.50 mmol), [Ir(COD)OMe]2 (2.5 mg, 0.00375 mmol) and 1a (3.8 mg, 0.0075 mmol) in THF (1.25 mL). The reaction was stirred at 50 °C for 20 hours before cooling and the solvents removed. Analysis of crude 1 H NMR using internal standard 1,2‐dimethoxyethane showed 16.8:1 meta:para borylation in 71% yield. The crude product was purified by silica gel chromatography (Pet. Ether (40‐60):EtOAc (9:1) to give the title compound as a white solid (60.5 mg, 0.17 mmol, 69%).

ORD 기록

ord-52ac8efd4b6f42b8acff3233e061b612

출처 데이터셋

Borylation dataset from Roche

DOI

10.1002/anie.201708967