Реакция #8577

Уравнение реакции

compound

(2S)-2-(2,3,4-Trifluoroanilino)-1-propanol

sodium hydride

→

title compound

Выход 66.5%

(3S)-(+)-7,8-Difluoro-3,4-dihydro-3-methyl-2H-[1,4]benzoxazine

Выход 66.5%

Растворители

DMF

DMF

Условия реакции

Обработка

1. 1
   workup.ADDITIONAfter treating in a conventional manner

Методика

To DMF (2 ml) was added sodium hydride (39 mg) and the mixture was heated to 60° C. in an oil bath. Next, a solution of the compound (100 mg) obtained in Example 51 in DMF was dropped therein to and the obtained mixture was stirred for 1 hour. After treating in a conventional manner, the mixture was subjected to silica gel column chromatography to give 60 mg (66%) of the title compound. The optical purity determined by HPCL was >94% ee. Various spectral data was identical with those of a specimen synthesized separately.

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