反应详情

A solution of 6-amino-4H-benzo[1,4]thiazin-3-one (10.68 g, 59.3 mmol; commercial) and (2R)-tert-butyl-dimethyl-(2-oxiranyl-ethoxy)-silane (first eluting compound of step C.i, 12.0 g, 59.3 mmol) in 9-1 EtOH/H2O (320 mL) was heated at 80° C. for 2 days. The mixture was concentrated under reduced pressure. Residual starting aniline could be removed by addition of Et2O/MeOH followed by filtration. The filtrate containing the product was concentrated under reduced pressure to afford the title intermediate as a brown oil (18.8 g, 83% yield) which was used as such in the next step.

1. concentrationThe mixture was concentrated under reduced pressure
2. customcould be removed by addition of Et2O/MeOH
3. filtrationfollowed by filtration
4. additionThe filtrate containing the product
5. concentrationwas concentrated under reduced pressure