反应详情

(2S,3R)-3-Ethylsulfanyl-2-(4′-fuoro-biphenyl-4-sulfonylamino)-3-phenyl-propionic acid. A mixture of (2S, 3R)-3-ethylsulfanyl-2-(4′-fluoro-biphenyl-4-sulfonylamino)-3-phenyl-propionic acid methyl ester 4b (28 mg, 0.059 mmol) and lithium iodide (105 mg, 0.785 mmol) in pyridine (3 mL) is refluxed under argon overnight. The mixture is cooled to room temperature and partitioned between ethyl acetate and 1.0 N aq. HCl. The organic layer is dried over Na2SO4, filtered, and concentrated under reduced pressure. The crude product is purified by reverse phase preparative HPLC (gradient elution, 0.1% aq. trifluoroacetic acid/acetonitrile) to give the desired product as a pale orange solid.

1. temperatureis refluxed under argon overnight
2. custompartitioned between ethyl acetate and 1.0 N aq. HCl
3. dry with materialThe organic layer is dried over Na2SO4
4. filtrationfiltered
5. concentrationconcentrated under reduced pressure
6. customThe crude product is purified by reverse phase preparative HPLC (gradient elution, 0.1% aq. trifluoroacetic acid/acetonitrile)