反应详情

To a 1/1 mixture of EtOH/EtOAc (50 mL each) was added concentrated HCl (12 M, 0.83 mL) to produce a 0.10 M solution. Solid 2(R)-benzyloxycarbonylamino-3-(morpholin-4-sulfonyl)-propionic acid benzyl ester (0.764 g, 1.65 mmol) was dissolved in this solution with gentle heating via heat gun until a clear colorless solution resulted. The solution was allowed to cool to rt with N2 aspiration, at which time 10% Pd/C (Aldrich, 0.300 g) was added in one portion to form a dark colored suspension. The reaction mixture was then shaken under an atmosphere of H2 (50 psi) in a Parr hydrogenator for 16 h. The suspension was filtered through a pad of celite, which is then washed with several portions of MeOH. The combined organics were concentrated in vacuo to afford 0.593 g (quant) of 2(R)-amino-3-(morpholin-4-sulfonyl)-propionic acid as its HCl salt as a solid orange foam.

1. temperaturewith gentle heating
2. temperaturevia heat gun until a clear colorless solution
3. customresulted
4. additionwas added in one portion
5. customto form a dark colored suspension
6. filtrationThe suspension was filtered through a pad of celite, which
7. washis then washed with several portions of MeOH
8. concentrationThe combined organics were concentrated in vacuo