4-((4-Methylpiperazin-1-yl)methyl)benzoyl Chloride Dihydrochloride is an intermediate in the synthesis of Gleevec N-4-((4-Methylpiperazin-1-yl)methyl)benzaldehyde (G407010), an impurity of Gleevec (G407000), a tyrosine kinase inhibitor which is highly specific for BCR-ABL, the enzyme associated with chronic myelogenous leukemia (CML) and certain forms of acute lymphoblastic leukemia (ALL).
Imaric acid 1g (5g, 0.021 mol, Anegi chemical) into 100mL three-necked bottle, add dichlorosulfoxide (35mL) and catalyst N, N-dimethylformamide (0.3mL), heating reflux reaction for 22 hours, reduced to room temperature, pumping and filtration, n-hexane washing (10mL 2), 45 ~ 50 C drying in vacuum for 2 hours, to obtain a white solid state of 4-(4- 4-(4-methylpiperazinylmethyl)benzoyl chloride dihydrochloride (1h) 5.1g, yield 95%.
