Continuously updated synthesis method about 4-Bromo-5-fluoro-2-iodoaniline

The synthetic route of 1219741-79-3 has been constantly updated, and we look forward to future research findings.

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. 1219741-79-3, name is 4-Bromo-5-fluoro-2-iodoaniline belongs to iodides-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below. Recommanded Product: 4-Bromo-5-fluoro-2-iodoaniline

To a vial was added, 4-bromo-5-fluoro-2-iodoaniline (5.67 g, 17.95 mmol), PdOAc2 (0.201 g, 0.897 mmol), sodium bicarbonate (3.77 g, 44.9 mmol), ethyl acrylate (2.049 ml, 18.85 mmol) and DMF (12.0 ml). The reaction was heated for 3 hour at 100 C. The reaction was cooled to RT, diluted with water and extracted with DCM (3*). The combined organics were washed with water and brine, dried over magnesium sulfate, filtered and concentrated. The resulting material was triturated with heptane overnight and then filtered to afford (E)-ethyl 3-(2-amino-5-bromo-4-fluorophenyl)acrylate (4.00 g, 13.88 mmol, 77% yield) as a light yellow solid. m/z (ESI) 288.0 (M+H)+.

The synthetic route of 1219741-79-3 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; Amgen Inc.; Weiss, Matthew; Boezio, Alessandro; Boezio, Christiane; Butler, John R.; Chu-Moyer, Margaret Yuhua; Dimauro, Erin F.; Dineen, Thomas; Graceffa, Russell; Guzman-Perez, Angel; Huang, Hongbing; Kreiman, Charles; La, Daniel; Marx, Isaac E.; Milgrim, Benjamin Charles; Nguyen, Hanh Nho; Peterson, Emily; Romero, Karina; Sparling, Brian; US9212182; (2015); B2;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com

Extracurricular laboratory: Synthetic route of 1219741-79-3

The synthetic route of 1219741-79-3 has been constantly updated, and we look forward to future research findings.

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. 1219741-79-3, name is 4-Bromo-5-fluoro-2-iodoaniline belongs to iodides-buliding-blocks compound, it is a common compound, a new synthetic route is introduced below. Safety of 4-Bromo-5-fluoro-2-iodoaniline

To a mixture of 4-bromo-5-fluoro-2-iodoaniline (step 1) (5.2 g, 16 mmol), Pd(PPh3)2Cl2 (582 mg, 0.83 mmol) and CuI (313 mg, 1.6 mmol) in 50 ml of Et3N was added ethynyltrimethylsilane (2.3 mL, 1.6 mmol) slowly at 0 C. The resulting mixture was degassed and charged with N2 three times. After stirring at 30 C. for 2 hrs, the reaction mixture was filtered over celite. The filtrate was diluted with ethyl acetate (*2), washed with water (*2) and brine (*2). The combined organic layers were dried over anhydrous Na2SO4 and filtered. The filtration was evaporated under reduced pressure to afford the crude product, which was purified by column chromatography on silica gel eluting with 0?5% ethyl acetate in hexanes to afford the title compound as yellow oil. LC-MS: Rt=1.29 mins; MS m/z [M+H]+ 286.0; Method 5-95AB 1.5minLC_v003 1H NMR (400 MHz, CDCl3) delta 7.19 (1H, d), 6.21 (1H, d), 4.11 (2H, s), 0.00 (9H, s).

The synthetic route of 1219741-79-3 has been constantly updated, and we look forward to future research findings.

Reference:
Patent; NOVARTIS AG; CHEN, Shuhui; HE, Haiyang; LAGU, Bharat; QIN, Hua; WU, Chengde; XIAO, Yisong; US2015/183802; (2015); A1;,
Iodide – Wikipedia,
Iodide – an overview | ScienceDirect Topics – ScienceDirect.com