Reference of 620621-48-9, These common heterocyclic compound, 620621-48-9, name is Methyl 2-chloro-5-iodobenzoate, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
Intermediate 2: Methyl 2-chloro-5-pyridin-2-ylbenzoate; A suspension of methyl 2-chloro-5-iodobenzoate (8.0 g, 27 mmol), 2- pyridineboronic acid N-phenyldiethanolamine ester (14.5 g, 54 mmol), palladium acetate (0.30 g, 1.35 mmol), potassium carbonate (7.46 g, 54.0 mmol), triphenylphosphine (1.42 g, 5.4 mmol) and copper iodide (2.06 g, 10.8 mmol) in THF (100 mL) was heated at 65 0C overnight under nitrogen. The reaction mixture was cooled, filtered through CeliteR and concentrated in vacuo, then the residue was suspended in DCM (250 mL) and filtered through Celite. The filtrate was concentrated in vacuo and the residue was purified by chromatography on silica gel eluting with EtOAc/isohexane (0 – 50%) to give the title
The synthetic route of 620621-48-9 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; AstraZeneca AB; AstraZeneca UK Limited; WO2009/47558; (2009); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com