ONE-POT SYNTHESIS OF 2-OXAZOLIDINONE DERIVATIVE

摘要

PROBLEM TO BE SOLVED: To provide a method for synthesizing (S)-4- [3-[2-(dimethylamino) ethyl]-1H-indol-5-yl]methyl}-2-oxazolidinone by an improved process. SOLUTION: This method for synthesizing the 2-oxazolidinone derivative includes the following steps: (a) a step for forming a carbamate of the formula (III) from methyl 4-nitro-(L)-phenylalaninate hydrochloride; (b) another step for reducing the compound of the formula (III) to obtain a compound of the formula (IV); (c) a third step for reducing a methyl ester group in the compound of the formula (IV) to obtain a compound of the formula (V); (d) a fourth step for subjecting the compound of the formula (V) to ring closure to obtain a compound of the formula (VI); (e) a fifth step for forming a diazonium salt from the compound of the formula (VI) and then reducing the diazonium salt to obtain a compound of the formula (VII); and the other step for subjecting the compound of the formula (VII) to Fischer's reaction to obtain the (S)-4- [3-[2-(dimethylamino)ethyl]-1H-indol-5-yl]methyl}-2-oxazolidinone.