反应详情

225 mg (0.664 mmol) of (rac.) 4-(3-chloro-2-methoxy-4-methylphenyl)-2-hydroxy-4-methyl-2-(trifluoromethyl)-pentanal, 106.3 mg (0.664 mmol) of 5-amino-isoquinolin-1(2H)-one, and 0.39 ml (1.328 mmol) of titanium tetraisopropylate are stirred in 3.6 ml of o-xylene for two and one-half hours at 120° C. After cooling, the batch is poured onto 15 ml of saturated brine and diluted with ethyl acetate. After 20 minutes of vigorous stirring at room temperature, it is filtered via a column, filled with Extrelute. The residue is on silica gel (mobile solvent ethyl acetate/hexane). 224.7 mg (70.3%) of the desired compound is isolated.

1. temperatureAfter cooling
2. filtrationit is filtered via a column
3. additionfilled with Extrelute