反应详情

温度

105 °C

A mixture of 250 mg (1.56 mmol) 3-methyl-1H-indazole-5-carbaldehyde (Example 1A), 328 mg (1.88 mmol) 3-(4-methoxyphenyl)-3-oxopropanenitrile and 128 mg (1.56 mmol) 3-aminobut-2-enenitrile in 1-pentanol (1.55 ml) containing powdered 4 Å molecular sieve was heated to 105° C. overnight. After cooling, the reaction mixture was diluted with acetonitrile and directly purified by preparative RP-HPLC (acetonitrile/water+0.1% TFA gradient) to afford 180 mg (30% of th.) of the racemic title compound.

1. additioncontaining
2. temperatureAfter cooling
3. customdirectly purified by preparative RP-HPLC (acetonitrile/water+0.1% TFA gradient)