反应详情

温度

100 °C

4-[5-(Chloromethyl)-1,3,4-oxadiazol-2-yl]-6-(1H-indol-4-yl)-1-(phenylsulfonyl)-1H-indazole (100 mg, 0.184 mmol) in acetonitrile (2 ml) was treated with 1-amino-3-(4-morpholinyl)-2-propanol (147 mg, 0.918 mmol, available from Enamine Ltd) and heated in a microwave at 100° C. for 30 mins. The solution was pipetted off the solid, then the solid was dissolved in DMSO (ml) and loaded onto a 5 g SCX cartridge. Methanol was eluted, then 2M ammonia in ethanol. Basic fractions were blown to dryness. The fully-protected intermediate was treated with isopropanol (1.000 ml) followed by 2M aqueous sodium hydroxide (1.001 ml, 2.002 mmol) and stirred for 20 h at 20° C. The solution was neutralised by addition of 2M hydrochloric acid then blown to dryness to give a brown solid. The material was purified MDAP (Method E). The appropriate fraction was blown to dryness to give the title compound as a brown film (27 mg).

1. washMethanol was eluted
2. additionThe fully-protected intermediate was treated with isopropanol (1.000 ml)
3. customto give a brown solid
4. customThe material was purified MDAP (Method E)