反应详情

A solution of 6-amino-4H-benzo[1,4]thiazin-3-one (10.68 g, 59.3 mmol; commercial) and tert-butyl-dimethyl-((R)-2-oxiranyl-ethoxy)-silane (as described in H.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 ether/MeOH followed by filtration. The mother liquor 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 ether/MeOH
3. filtrationfollowed by filtration
4. additionThe mother liquor containing the product
5. concentrationwas concentrated under reduced pressure