Reaktion #60702

ord-d31465e065a0431c8898384061e601d0

Reaktionsgleichung

O=C(NC(COCC1CCNCC1)c1ccccc1Cl)c1ccc2c(Cl)c[nH]c2c1
3-chloro-N-[1-(2-chloro-phenyl)-2-(piperidin-4-ylmethoxy)ethyl]-1H-indole-6-carboxamide
C=O
paraformaldehyde
→
CN1CCC(COCC(NC(=O)c2ccc3c(Cl)c[nH]c3c2)c2ccccc2Cl)CC1
3-Chloro-N-[1-(2-chlorophenyl)-2-(1-methylpiperidin-4-yl-methoxy)ethyl]-1H-indole-6-carboxamide

Edukte

O=C(NC(COCC1CCNCC1)c1ccccc1Cl)c1ccc2c(Cl)c[nH]c2c1
3-chloro-N-[1-(2-chloro-phenyl)-2-(piperidin-4-ylmethoxy)ethyl]-1H-indole-6-carboxamide
C=O
paraformaldehyde

Reagenzien

Keine

Reaktionsbedingungen

Detaillierte Bedingungen
See reaction.notes.procedure_details.

Aufarbeitung

  1. 1
    Sonstigeafforded
  2. 2
    Sonstigeafter purification (SiO2: 10:10:1 hexane:EtOAc:isopropylamine), 175 mg (57%) of the title compound

Vorschrift

Using alkylation method B, 3-chloro-N-[1-(2-chloro-phenyl)-2-(piperidin-4-ylmethoxy)ethyl]-1H-indole-6-carboxamide (300 mg, 0.67 mmol) and paraformaldehyde (201 mg, 6.7 mmol) afforded, after purification (SiO2: 10:10:1 hexane:EtOAc:isopropylamine), 175 mg (57%) of the title compound.

Quelle

DOI: 10.6084/m9.figshare.5104873.v1Patent: US07427632B2uspto-grants-2008_09