Reaktion #682004

ord-756aa8ca2bc64aa089e280ef8856ba8d

Lösungsmittel

Reaktionsbedingungen

Detaillierte Bedingungen
See reaction.notes.procedure_details.

Aufarbeitung

  1. 1
    EinengenThereafter, the reaction solution was concentrated in vacuo
  2. 2
    workup.DISSOLUTIONthe obtained residue was then dissolved in chloroform
  3. 3
    WaschenThe obtained solution was washed with a saturated aqueous solution of sodium hydrogen carbonate
  4. 4
    Trocknenwas then dried over sodium sulfate
  5. 5
    Einengenwas then concentrated in vacuo

Vorschrift

The (S)-tert-butyl 3-((R)-2-(4-(cyclopropylsulfonyl)phenyl)-3-((5-fluorothiazol-2-yl)amino)-3-oxopropyl)pyrrolidine-1-carboxylate (2.57 g, 4.91 mmol) obtained in Example 1 was dissolved in hydrochloric acid (4 M ethyl acetate solution, 10 mL), and the obtained mixture was then stirred for 10 minutes. Thereafter, the reaction solution was concentrated in vacuo, and the obtained residue was then dissolved in chloroform. The obtained solution was washed with a saturated aqueous solution of sodium hydrogen carbonate, was then dried over sodium sulfate, and was then concentrated in vacuo, so as to obtain (R)-2-(4-(cyclopropylsulfonyl)phenyl)-N-(5-fluorothiazol-2-yl)-3-((S)-pyrrolidin-3-yl)propanamide (2.26 g, quant) in the form of a white solid.

Quelle

DOI: 10.6084/m9.figshare.5104873.v1Patent: US09242978B2uspto-grants-2016_01