反应详情

[(S)-1-(3-Hydroxy-azepan-4-ylcarbamoyl)-3-methyl-butyl]-carbamic acid-tert-butyl ester (compound 2g, 0.8 g, 2.33 mmol) was dissolved in 1,2-dichloroethane (DCE, 20 ml). Then, morpholinemethyl polystyrene resin beads (1.26 g, 3.7 mmol/g, Nova) were added and the solution was shaken for 5 minutes. Then, p-methoxybenzenesulfonyl chloride (0.48 g, 2.33 mmol) was dissolved in DCE (10 ml), and this solution was added to the reaction mixture. The reaction was shaken overnight, filtered, washed with DCE (2×10 ml), then CH2Cl2 (10 ml). The combined organics were concentrated in vacuo, and used in the next reaction without further purification: M+H+=514.2.

1. additionwere added
2. additionthis solution was added to the reaction mixture
3. stirringThe reaction was shaken overnight
4. filtrationfiltered
5. washwashed with DCE (2×10 ml)
6. concentrationThe combined organics were concentrated in vacuo
7. customused in the next reaction without further purification