4-(2-Propyn-1-yl)morpholine → 1-(3,5-Dichloro-pyridin-4-ylmethyl)-6-methoxy-5-(3-morpholin-4-yl-prop-1-ynyl)-phthalazine

Participants

Reaction Steps

Operating analogously to what described in example 74 starting from trifluoro-methanesulfonic acid 1-(3,5-dichloro-pyridin-4-ylmethyl)-6-methoxy-phthalazin-5-yl ester (2 g, 4.27 mmoles), prepared as described in example 73, 4-prop-2-ynyl-morpholine (640 mg, 5.12 mmoles), prepared as described in example 137, diethylamine (40 ml), bis(triphenylphosphine)PdCl2 (60 mg, 0.0854 mmole) and Cul (16 mg, 0.0854 mmole), 728 mg of the title compound were obtained (yield: 38.6%).

Provenance & Evidence