Reaktion #40359

ord-5891a95dbe0a4f5487ba99d0197a9015

Reaktionsbedingungen

Detaillierte Bedingungen
See reaction.notes.procedure_details.

Aufarbeitung

  1. 1
    workup.ADDITIONwere added
  2. 2
    TemperaturThe reaction mixture was refluxed for 2 hrs
  3. 3
    Einengenconcentrated in vacuo
  4. 4
    Sonstigewas evaporated
  5. 5
    Sonstigeyielded 280 mg (89%) with a purity of 87%

Vorschrift

To a mixture of 252 mg (0.7 mmol) of [4-(4-Amino-2,5-dimethyl-phenoxy)-pyrimidin-2-yl]-methyl-phenyl-amine and 4 ml of trimethoxymethane, 20 mg of p-toluene sulfonic acid were added. The reaction mixture was refluxed for 2 hrs and concentrated in vacuo. The mixture was solved in 10 ml of dichloromethane and 62 mg (1.05 mmol) methyl ethyl amine was added. After stirring 18 hrs at ambient temperature the mixture was evaporated and yielded 280 mg (89%) with a purity of 87%; log P (pH 2.3)=1.61.

Quelle

DOI: 10.6084/m9.figshare.5104873.v1Patent: US07727986B2uspto-grants-2010_06