反应详情

To a solution of 2-(2-(3-(morpholin-4-yl)-n-propyl)aminoanilin-4-yl)benzoxazole (see Working Example 96-1) (300 mg, 0.851 mmol) in methanol (5 mL) was added methyl acetimidate hydrochloride (103 mg, 0.936 mmol), and this was heated to reflux for 3 hours. After the reaction was complete, saturated aqueous sodium hydrogen carbonate solution was added, and this was extracted with ethyl acetate. After the organic layer obtained was dried over anhydrous sodium sulfate, it was filtered and concentrated. To the crystals obtained was added diethyl ether, this was filtered, washed with diethyl ether, and dried to yield the title compound (195 mg, 61% yield) as light brown crystals.

1. temperaturethis was heated
2. temperatureto reflux for 3 hours
3. extractionthis was extracted with ethyl acetate
4. customAfter the organic layer obtained
5. dry with materialwas dried over anhydrous sodium sulfate, it
6. filtrationwas filtered
7. concentrationconcentrated
8. customTo the crystals obtained
9. filtrationthis was filtered
10. washwashed with diethyl ether
11. customdried