亦然高效酰胺化试剂----TCFH−NMI

anamide (6a): The (S)-2-phenylpropionic acid (S)-5 (0.45 mL, 3.23 mmol, 1.0 equiv), 0.47 g 4-aminobenzonitrile 2a (3.87 mmol, 1.2 equiv), 0.54 mL N-methylimidazole (6.78 mmol, 2.1 equiv) were combined and dissolved in 10 mL MeCN for addition of the 1.0 g of TCFH (3.55 mmol, 1.1 equiv) in a single portion. The reaction was stirred until complete by HPLC (30 min). The reaction was then diluted with 20 mL isopropyl acetate and 20 mL of water. The layers were separated, dried over Na2SO4, filtered and concentrated before purification by silica gel chromatography with heptane/ethyl acetate to give 749 mg of 6a as a white solid (93% yield).3 Direct isolation of the desired amide could be achieved through addition of 4-6 mL water, filtration and washing with 5 mL of 2:1 water/MeCN before drying under nitrogen without a significant change in yield. Reported yields represent those obtained by chromatography for consistency and to oid enrichment through crystallization. TLC Rf = 0.29 (7:3 heptane/EtOAc, UV 254 nm).

参考资料：

TCFH–NMI: Direct Access to N-Acyl Imidazoliums for Challenging Amide Bond Formations， Org. Lett. 2018, 20, 14, 4218–4222.

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