In the next few decades, the world population will flourish. As the population grows rapidly and people all over the world use more and more resources, all industries must consider their environmental impact. 391211-97-5, name is 3,4-Difluoro-2-((2-fluoro-4-iodophenyl)amino)benzoic acid belongs to iodides-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below. Application In Synthesis of 3,4-Difluoro-2-((2-fluoro-4-iodophenyl)amino)benzoic acid
A solution of 3,4-difluoro-2-[(2-fluoro-4-iodophenyl)amino]benzoic acid (200 mg, 0.51 mmol), prepared using procedures similar to those in US 7,019,033, PyBOP (256 mg, 0.51 mmol), commercially available tert-butyl azetidin-3-ylcarbamate (131 mg, 0.77 mmol) and lambdazetaiV-diisopropylethylamine (180 muL, 1.02 mmol) in dimethylformamide (3 mL) was stirred at room temperature for 15 hours. The reaction mixture was partitioned between 5% aqueous lithium chloride and ethyl acetate. The organic portion was washed with 20% aqueous citric acid, saturated aqueous sodium bicarbonate, brine, dried over sodium sulfate, filtered and concentrated in vacuo to afford a brown residue which was purified by silica gel column chromatography eluting with 30% ethyl acetate in hexanes to afford 1,1- dimethylethyl [ 1 -( { 3 ,4-difluoro-2- [(2-fluoro-4-iodophenyl)amino]phenyl } carbonyl)azetidin- 3-yl]carbamate (225 mg, 80% yield) as a colorless oil. 1H NMR (400 MHz, DMSO): 8.56 (s, IH), 7.60-7.55 (m, 2H), 7.38 (d, IH), 7.30-7.26 (m, IH), 7.20-7.13 (m, IH), 6.71-6.66 (m, IH), 4.37-4.20 (m, 2H), 4.18-4.06 (m, IH), 3.98-3.93 (m, IH), 3.82-3.75 (m, IH), 1.37 (s, 9H). MS (EI) C2IH21N3O3F3I: 548 (MH+).
The synthetic route of 391211-97-5 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; EXELIXIS, INC.; WO2008/124085; (2008); A2;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com