abstract |
The present invention relates to a kind of novel quinazoline compound and the method for using it to prepare the quinazoline crotyl compound used for treating or preventing various indications related to EGFR and HER2 kinase function. The raw material reacts with diethylphosphonoacetic acid and N,N'-carbonyldiimidazole in a solvent at a temperature of 25~50°C to convert the amino group in the raw material into diethylphosphoracetamide group, and then react the intermediate with N , N'-disubstituted acetaldehyde reacts in a solvent, in the presence of alkaline substances, and at a temperature of -30°C~-20°C to generate the target compound. The route adopted by the present invention can obtain the target product with a purity greater than 98% through simple post-treatment, and the total yield of the target product is as high as 74%. In addition, the method of the present invention has successfully achieved the preparation of the target product at the kilogram level, and is easy to produce in batches. |