反应详情

According to Scheme 19 Step 1: The title compound was prepared from 1-(4-chloro-2-fluorobenzyl)-5-bromopyridin-2(1H)-one (1 eq, 2.81 mmol, 0.89 g, Example 1 Step 2) and 4-(tert-butoxycarbonyl)aminophenylboronic acid (1.5 eq, 4.20 mmol, 1.00 g) according to the procedure described for Example 1 Step 3. Reaction conditions: 2 hours at 80° C. The crude product was purified by silica gel chromatography (AIT Flashsmart prepacked column 50 g SiO2, CH2Cl2/AcOEt 90/10). The resulting brown solid washed twice with acetonitrile to afford tert-butyl 4-(1-(4-chloro-2-fluorobenzyl)-6-oxo-1,6-dihydropyridin-3-yl)phenylcarbamate (2.11 mmol, 0.90 g, 75%) as a beige solid.

1. customReaction conditions
2. custom2 hours
3. customat 80° C
4. customThe crude product was purified by silica gel chromatography (AIT Flashsmart prepacked column 50 g SiO2, CH2Cl2/AcOEt 90/10)
5. washThe resulting brown solid washed twice with acetonitrile