HCID 86717954, Verbindung → HCID 86717953, Verbindung

HRID 2275879Notizen

Reaktionsgleichung

Reaktionsgleichung von HRID 2275879
[F:1][C:2]1[CH:37]=[CH:36][CH:35]=[C:34]([F:38])[C:3]=1[CH2:4][O:5][C:6]1[C:7]2[N:8]([C:12]([C:16]([NH:18][C@H:19]3[CH2:23][CH2:22][N:21](C(OCC4C=CC=CC=4)=O)[CH2:20]3)=[O:17])=[C:13]([CH3:15])[N:14]=2)[CH:9]=[CH:10][CH:11]=1>C(O)C.[OH-].[Pd+2].[OH-]>[F:1][C:2]1[CH:37]=[CH:36][CH:35]=[C:34]([F:38])[C:3]=1[CH2:4][O:5][C:6]1[C:7]2[N:8]([C:12]([C:16]([NH:18][C@H:19]3[CH2:23][CH2:22][NH:21][CH2:20]3)=[O:17])=[C:13]([CH3:15])[N:14]=2)[CH:9]=[CH:10][CH:11]=1

Komponenten

4

Edukt 1

HCID 86717954HCID 86717954, Verbindung

Produkt 1

HCID 86717953HCID 86717953, Verbindung

Reagenzien, Katalysatoren, Lösungsmittel 2

HCID 9942167Palladium hydroxideKatalysatorHCID 702EthanolLösungsmittel

Versuchsvorschrift

130 mg of benzyl (3S)-3-[({8-[(2,6-difluorobenzyl)oxy]-2-methylimidazo[1,2-a]pyridin-3-yl}-carbonyl)amino]pyrrolidine-1-carboxylate (Example 115A; 0.250 mmol) were initially charged in 60 ml of ethanol, 17.5 mg 20% palladium-(II) hydroxide (0.025 mmol, 0.1 equivalents) were added and the mixture was hydrogenated under hydrogen standard pressure for two hours. The reaction mixture was filtered and concentrated and the residue was purified by preparative HPLC. This gave 42 mg (44% of theory) of the title compound.

Aufarbeitung

  1. customfor two hours
  2. filtrationThe reaction mixture was filtered
  3. concentrationconcentrated
  4. customthe residue was purified by preparative HPLC

Quellen und Nachweise

ORD-Eintrag
ord-513e193950ce4b0e9eb88a00346a7b5a
Quelldatensatz
uspto-grants-2015_09
Patentnummer
US09126998B2

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