3-Pyridinemethanamine → HCID 24948342, compound

Participants

Reaction Steps

A mixture 6-bromo-4-chloro-2H-phthalazin-1-one (150 mg, 0.578 mmol), 3-(aminomethyl)pyridine (0.064 mL, 0.636 mmol), Pd2(dba)3 (53 mg, 0.058 mmol), rac-BINAP (115 mg, 0.185 mmol) and NaOtBu (169 mg, 1.759 mmol) in DMA (5 mL) was heated at 85° C. for 2 h. The mixture was allowed to cool, then filtered. Preparatory HPLC afforded 4-chloro-6-[(pyridin-3-ylmethyl)-amino]-2H-phthalazin-1-one hydroformate (31 mg) as a yellow solid, 1H (400 MHz, d6-DMSO) δ: 4.41 (d, 2H), 6.78 (d, 1H), 7.12 (dd, 1H), 7.31 (dd, 1H), 7.60 (t, 1H), 7.10 (m, 1H), 7.88 (d, 1H), 8.09 (s, 1H), 8.41 (dd, 1H), 8.56 (d, 1H), 12.31 (s, 1H) ppm; m/z (M+1) 286.99.

Provenance & Evidence