تفاعل #163083

معادلة التفاعل

N-(5-cyclopropyl-1H-pyrazol-3-yl)-3,6-difluoropyridin-2-amine

(S)—N6-(5-Cyclopropyl-1H-pyrazol-3-yl)-N2-(1-(4-fluorophenyl)ethyl)pyridine-2,3,6-triamine

(S)-1-(4-fluorophenyl)ethanamine

→

title compound

المردود 26.8%

(S)—N2-(5-Cyclopropyl-1H-pyrazol-3-yl)-3-fluoro-N6-(1-(4-fluorophenyl)ethyl)pyridine-2,6-diamine

المردود 26.8%

ظروف التفاعل

المعالجة

1. 1
   أخرىThe resulting dark oil was purified by column chromatography (DCM-MeOH=80:1)

الإجراء التجريبي

A mixture of N-(5-cyclopropyl-1H-pyrazol-3-yl)-3,6-difluoropyridin-2-amine (Method 31, 0.10 g, 0.42 mmol) and (S)-1-(4-fluorophenyl)ethanamine (0.3 g, 2.2 mmol) were heated to 185° C. under microwave conditions (30 min×3 cycles). The resulting dark oil was purified by column chromatography (DCM-MeOH=80:1) to give the title compound (0.04 g, 26%). 1H NMR (400 MHz, CD3OD) δ 7.08-6.99 (m, 3H), 6.67-6.62 (m, 2H), 6.22 (dd, J=8.9, 2.3 Hz, 1H), 5.04 (s, 1H), 4.64-4.59 (m, 1H), 1.16-1.12 (m, 4H), 0.30-0.14 (m, 3H), 0.04-0.02 (m, 1H). MS: Calcd.: 355. Found: [M+H]+ 356.

المصدر