Cyclobutylamine → HCID 46192529, compound

Participants

Reaction Conditions

Reaction Steps

2,4,5-trichloro-pyrimidine (0.5 M in DMSO) cyclobutyl amine (0.5 M in DMSO, 160 μL) and DIEA (neat, 30 μL) were added to an 8-ml reaction vial. The vial was capped and the contents shaken at 25° C. for 22 h. The reaction mixture was concentrated in Genevac to provide 4-cyclobutylamino-2,5-dichloro-pyrimidine. The solid was treated with C16 (0.5 M in DMSO, 160 μL), concentrated in Genevac, and the resultant residue treated with EtOAc (160 ul). The vial was capped and the contents shaken at 75° C. for 22.5 hours. The reaction mixture was then concentrated in Genevac. The resultant crude product was dissolved in DMSO and purified by HPLC to provide 418 (11.9 mg, 35%). APCI LCMS: Retention time: 3.00 min (Method A), Observed mass: 419.99 [M+H].

Provenance & Evidence