tert-butyl 2-(methylsulfanyl)-4,5-dihydro-1H-imidazole-1-carboxylate → 2-[3-Cyano-5-methyl-4-(4-phenoxy-phenylamino)-pyrrolo[1,2-b]pyridazin-6-ylamino]-4,5-dihydro-imidazole-1-carboxylic acid tert-butyl ester

Beteiligte Stoffe

Reaktionsbedingungen

Reaktionsschritte

A mixture of 6-amino-5-methyl-4-(4-phenoxy-phenylamino)-pyrrolo[1,2-b]pyridazine-3-carbonitrile hydrochloride (Example 11) (49 mg, 0.125 mmol) and 2-methylsulfanyl-4,5-dihydro-imidazole-1-carboxylic acid tert-butyl ester (25.5 mg, 0.125 mmol) in MeOH (2 ml) was heated at 70° C. for 3 h, then cooled to rt and stirred overnight. The reaction mixture was diluted with CHCl3 (25 ml), washed with saturated NaHCO3 (10 ml) dried with Na2SO4. Concentrated in vacuo and purified by prep. TLC to give 424A (22 mg, 97%) as pale yellow flakes (5% MeOH—CHCl3). It has a retention time of 6.82 min (standard LC1 method, 8 min run). MS Found: (M+M)+=523.9

Herkunft & Nachweise