2-[4-(Morpholin-4-yl)-2-(1-tert-butoxycarbonylpiperidin-4-yloxy)benzoylamino]-N-(5-chloropyridin-2-yl)benzamide → N-(5-Chloropyridin-2-yl)-2-[4-(morpholin-4-yl)-2-(piperidin-4-yloxy)-benzoylamino]benzamide

HRID 644171

Reaktionsgleichung

Reaktionsgleichung von HRID 644171
[N:1]1([C:7]2[CH:31]=[CH:30][C:10]([C:11]([NH:13][C:14]3[CH:29]=[CH:28][CH:27]=[CH:26][C:15]=3[C:16]([NH:18][C:19]3[CH:24]=[CH:23][C:22]([Cl:25])=[CH:21][N:20]=3)=[O:17])=[O:12])=[C:9]([O:32][CH:33]3[CH2:38][CH2:37][N:36](C(OC(C)(C)C)=O)[CH2:35][CH2:34]3)[CH:8]=2)[CH2:6][CH2:5][O:4][CH2:3][CH2:2]1>C(O)(C(F)(F)F)=O>[Cl:25][C:22]1[CH:23]=[CH:24][C:19]([NH:18][C:16](=[O:17])[C:15]2[CH:26]=[CH:27][CH:28]=[CH:29][C:14]=2[NH:13][C:11](=[O:12])[C:10]2[CH:30]=[CH:31][C:7]([N:1]3[CH2:2][CH2:3][O:4][CH2:5][CH2:6]3)=[CH:8][C:9]=2[O:32][CH:33]2[CH2:38][CH2:37][NH:36][CH2:35][CH2:34]2)=[N:20][CH:21]=1

Komponenten

3

Edukt 1

HCID 685307202-[4-(Morpholin-4-yl)-2-(1-tert-butoxycarbonylpiperidin-4-yloxy)benzoylamino]-N-(5-chloropyridin-2-yl)benzamide

Produkt 1

HCID 57860933N-(5-Chloropyridin-2-yl)-2-[4-(morpholin-4-yl)-2-(piperidin-4-yloxy)-benzoylamino]benzamideAusbeute 100 %

Reagenzien, Katalysatoren, Lösungsmittel 1

HCID 6422Trifluoroacetic acidLösungsmittel

Versuchsvorschrift

The 2-[4-(morpholin-4-yl)-2-(1-tert-butoxycarbonylpiperidin-4-yloxy)-benzoylamino]-N-(5-chloropyridin-2-yl)benzamide (164 mg, 0.26 mmol) was dissolved in TFA (3 mL). After 5 minutes, the reaction was concentrated in vacuo. The residue was diluted with methylene chloride (100 mL) and washed with saturated aqueous sodium carbonate. The organic layer was dried over sodium sulfate, filtered, and concentrated to give the desired product (138 mg, 0.26 mmol, 100%).

Aufarbeitung

  1. concentrationthe reaction was concentrated in vacuo
  2. additionThe residue was diluted with methylene chloride (100 mL)
  3. washwashed with saturated aqueous sodium carbonate
  4. dry with materialThe organic layer was dried over sodium sulfate
  5. filtrationfiltered
  6. concentrationconcentrated

Quellen und Nachweise

ORD-Eintrag
ord-28659d2b8566450fbd579d3fca1e141d
Quelldatensatz
uspto-grants-2010_04
Patentnummer
US07700628B2

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