Introduction of a new synthetic route about 4-Fluoro-2-iodobenzoic acid

According to the analysis of related databases, 4-Fluoro-2-iodobenzoic acid, the application of this compound in the production field has become more and more popular.

56096-89-0, In the chemical reaction process, reaction time, type of solvent, can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product. An updated downstream synthesis route of 56096-89-0 as follows.

In a MW tube was added 4-fluoro-2-iodobenzoic acid (600 mg, 1.88 mmol), 1 H-1 ,2,3- Triazole (0.22 ml_, 3.76 mmol) and (1 R,2R)-N 1 ,N2-dimethylcyclohexane-1 ,2-diamine (0.06 ml_, 0.38 mmol). To these solids were added 1 ,4-Dioxane (2 ml_) and Water (0.2 ml_), then Cul (18 mg, 0.09 mmol) and finally Cs2C03 (1 .22 g, 3.76 mmol). The mixture was then warmed to 100 C for 2.5 hrs and left at RT O/N . HCI 6 N was added until pH 2, then volatiles were removed under vacuum and the crude material was purified by RP on C18 column (from H20/CH3CN 95:5 + 0.1 % of FA to H20/CH3CN 5:95 + 0.1 % of FA) affording 4-fluoro-2-(2H-1 ,2,3-triazol-2-yl)benzoic acid (p185, 250 mg, y= 64%) as white solid. MS (m/z): 206.3 [M-H]”

According to the analysis of related databases, 4-Fluoro-2-iodobenzoic acid, the application of this compound in the production field has become more and more popular.

Reference:
Patent; CHRONOS THERAPEUTICS LIMITED; MICHELI, Fabrizio; BERTANI, Barbara; GIBSON, Karl Richard; DI FABIO, Romano; RAVEGLIA, Luca; ZANALETTI, Riccardo; CREMONESI, Susanna; POZZAN, Alfonso; SEMERARO, Teresa; TARSI, Luca; LUKER, Timothy Jon; (275 pag.)WO2019/43407; (2019); A1;,
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