Reaction #554645

ord-58504ec6bfcd49f6b2ce6311b2794191

Reaction equation

Clc1ncc(Br)cn1
5-bromo-2-chloropyrimidine
NC1CCC1
cyclobutylamine
CCN(C(C)C)C(C)C
DIPEA
CC#N
ACN
Brc1cnc(NC2CCC2)nc1
5-Bromo-N-cyclobutylpyrimidin-2-amine

Solvents

Conditions

Temperature
50°CELSIUS
Detailed conditions
See reaction.notes.procedure_details.

Workup

  1. 1
    Washwashed with water (2×)
  2. 2
    Dryingphase is dried with MgSO4
  3. 3
    Filtrationfiltered
  4. 4
    Otherthe solvent is removed in vacuo

Procedure

In a sealed tube 2.00 g (10.3 mmol) 5-bromo-2-chloropyrimidine, 1.15 mL (13.4 mmol) cyclobutylamine and 2.70 mL (15.5 mmol) DIPEA are added to 12 mL ACN. The reaction mixture is stirred at 50° C. over night, then diluted with EtOAc and washed with water (2×). The org. phase is dried with MgSO4, filtered and the solvent is removed in vacuo.

Source

DOI: 10.6084/m9.figshare.5104873.v1Patent: US08623860B2uspto-grants-2014_01