反应详情

The product can be prepared as described in stage 2 of Example 12, but using 465 mg of N-(4,5-difluoro-2-hydroxyphenyl)-2-[4-(morpholin-4-yl)-6-oxo-1,6-dihydropyrimidin-2-yl]acetamide in 30 ml of xylene and 77 mg of 4-methylbenzenesulphonique acid hydrate. After refluxing for six hours, addition of 100 mg of 4-methylbenzenesulphonic acid hydrate and purification by silica column chromatography, eluent: gradient of pure CH2Cl2 to CH2Cl2/MeOH: 96/04, the product obtained is taken up with 20 ml of diethyl ether and then spin-filter-dried and dried under vacuum. 63 mg of 2-[(5,6-difluoro-1,3-benzoxazol-2-yl)methyl]-6-(morpholin-4-yl)pyrimidin-4(3H)-one are obtained in the form of a white solid, the characteristics of which are the following:

1. customThe product can be prepared
2. temperatureAfter refluxing for six hours
3. customspin-filter-dried
4. customdried under vacuum