Some tips on 4-Fluoro-2-iodoaniline

The synthetic route of 61272-76-2 has been constantly updated, and we look forward to future research findings.

61272-76-2, name is 4-Fluoro-2-iodoaniline, belongs to iodides-buliding-blocks compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. COA of Formula: C6H5FIN

7V-Benzyl-5-bromo-2-iodobenzamide (125 mg, 0.30 mmol), 4-fluoro-2-iodoaniline (29 pL, 0.25 mmol), copper(I) iodide (10 mg, 0.05 mmol), and potassium carbonate (86 mg, 0.63 mmol) were taken up in anhydrous DMSO (1.5 mL). The resulting reaction mixture was first stirred at 80 C for 2 hr, followed by heating to 135 C for another 10 hr. After cooling to room temperature, the mixture was diluted with an excess of Et20 and washed with water. The organic layer was dried over NaiSGy filtered and concentrated. The residue was purified by flash column chromatography (EtOAc : Hex = 0 : 100 to 100 : 0; EtOAc : DCM = 0 : 100 to 30 : 70) to give 10-benzyl-2-bromo-8-fluoro-5,10-dihydro-l li7-dibenzo[Z>,e][l,4]diazepin-l l-one (43 mg, 44 %) as a light yellow solid. (0794) NMR (500 MHz, DMSO-de) d 8.06 (s, 1H), 7.74 (d, J = 2.4 Hz, 1H), 7.54 (dd, J = (0795) 2.4, 8.5 Hz, 1H), 7.30 – 7.24 (m, 5H), 7.22 – 7.17 (m, 1H), 7.09 (dd, J= 6.0, 8.7 Hz, 1H), 7.04 (d, ./ 8.9 Hz, 1 H), 6.91 (td, J= 2.7, 8.4 Hz, 1H), 5 26 (s, 2H); LC/MS (ESI) m/z 396.73 [M+H]+.

The synthetic route of 61272-76-2 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; DANA-FARBER CANCER INSTITUTE, INC.; GRAY, Nathanael S.; DE CLERCQ, Dries; JANG, Jaebong; JANNE, Pasi; TO, Ciric; ECK, Michael; PARK, Eunyoung; HEPPNER, David; (0 pag.)WO2019/164949; (2019); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com