2-([1,2,4]Triazolo[1,5-a]pyridin-2-yl)ethanamine → 2-(2-([1,2,4]Triazolo[1,5-A]pyridin-2-YL)ethyl)-7-chloro-5-methyl-2,3-dihydro-1H-pyrrolo[3,4-C]pyridine-1,6(5H)-dione

Participants

Reaction Conditions

Reaction Steps

TEA (3.01 ml, 21.59 mmol) was added rapidly to a solution of 2-([1,2,4]triazolo[1,5-a]pyridin-2-yl)ethanamine (1.167 g, 7.20 mmol) and 1-methyl-2-oxo-1,2-dihydro-3-chloro-4-methoxycarbonyl-5-chloromethyl-pyridine (1.8 g, 7.20 mmol, see compound (6) of Example b1)) in MeCN (15 ml). The reaction was heated in a microwave at about 100° C. for about 40 min. The reaction was cooled to r.t. and the mixture was filtered through a Büchner funnel. The residue solid was triturated with water (2×20 ml). The resulting solid was filtered off on a Büchner funnel to afford the title compound (1.3 g, 3.78 mmol, 52.5% yield).

Provenance & Evidence