반응 #67781

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3-[(4-iodo-2-methylphenyl)amino]isonicotinic acid

3-[(4-Iodo-2-methylphenyl)amino]isonicotinic acid

DIPEA

O-ethylhydroxylamine hydrochloride

→

desired product

수율 53.0%

N-Ethoxy-3-[(4-iodo-2-methylphenyl)amino]isonicotinamide

수율 53.0%

용매

DMF

반응 조건

후처리

1. 1
   기타the volatiles were removed in vacuo
2. 2
   기타The crude material was purified by preparative reversed phase HPLC

실험 절차

3-[(4-iodo-2-methylphenyl)amino]isonicotinic acid 2c (60 mg, 0.17 mmol) was dissolved in 6 ml dry DMF followed by the addition of DIPEA (0.20 mmol, 37 μl), ByBOP (0.20 mmol, 107 mg) and O-ethylhydroxylamine hydrochloride (0.34 mmol, 34 mg). The mixture was stirred for 4 h and the volatiles were removed in vacuo. The crude material was purified by preparative reversed phase HPLC to give 36 mg (91 μmol; 53% yield) of pure desired product.

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