These common heterocyclic compound, 74534-15-9, name is 1-Chloro-2-iodo-4-nitrobenzene, 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. name: 1-Chloro-2-iodo-4-nitrobenzene
A dried round flask charged with 1-chloro-2-iodo-4-nitrobenzene (17.0 g, 60 mmol), 3,5-dimethylisoxazol-4-ylboronic acid (25.4 g, 180 mmol), Pd(Ph3P)4 (3.47 g, 3.0 mmol) and Ba(OH)28H20 (37.9 g, 120 mmol) in DME (315 mL) and water (93 mL) was evacuated and refilled with N2 gas in several times. The reaction mixture was stirred at 80 C for 16 hours, cooled to room temperature and quenched with water. The mixture wasextracted with EtOAc twice. The combined organic layers were dried over MgSO4, filtered and concentrated in vacuo. The residue was purified by column chromatography on Si02 (Hex/EtOAc = 9:1) to afford the titled compound (5.5 g, 36%) as a yellow solid.?H-NMR (400 MHz, CDC13): oe 8.20 (dd, J 8.4, 2.0 Hz, 1H), 8.09 (d, J= 2.0 Hz, 1H), 7.68 (d, J= 8.4 Hz, 1H), 2.31 (s, 3H), 2.16 (s, 3H).
The synthetic route of 1-Chloro-2-iodo-4-nitrobenzene has been constantly updated, and we look forward to future research findings.
Reference:
Patent; KAINOS MEDICINE, INC.; CHOI, Minjeong; OH, Su-Sung; (113 pag.)WO2016/186453; (2016); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com