Reaktion #48375

ord-1864fc320c9f4b4f8d973168c4ef18c9

Lösungsmittel

Reaktionsbedingungen

Detaillierte Bedingungen
See reaction.notes.procedure_details.

Aufarbeitung

  1. 1
    Einengenthe reation was concentrated
  2. 2
    workup.ADDITIONdiluted with dichlormethane (5 mL)
  3. 3
    workup.ADDITIONa solution of 1N hydrochloric acid in 1,4-dioxane (2 mL) was added at room temperature
  4. 4
    EinengenConcentration

Vorschrift

tert-Butyl 4-(6-fluoro-2-oxo-2,3-dihydro-1H-imidazo[4,5-b]pyridin-1-yl)piperidine-1-carboxylate (340 mg, 1.01 mmol) was dissolved in dichloromethane (5 mL) and trifluoroacetic acid (5 mL) was added. After 2 h, the reation was concentrated, diluted with dichlormethane (5 mL) and a solution of 1N hydrochloric acid in 1,4-dioxane (2 mL) was added at room temperature. Concentration afforded the title compound (302 mg). MS 237.2 (M+1) 1H NMR (500 MHz, CDODl3) δ 7.92 (br s, 1H), 7.70 (dd, 1H), 4.60 (m, 1H), 3.60 (s, 2H), 3.25 (dd, 2H), 2.70 (m, 2H), 2.10 (d, 2H).

Quelle

DOI: 10.6084/m9.figshare.5104873.v1Patent: US07745427B2uspto-grants-2010_06