Application of 1020198-58-6, These common heterocyclic compound, 1020198-58-6, name is 2-Bromo-1-chloro-3,5-difluorobenzene, 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.
Example 93 Preparation of Compound 93 (lR,4S,12aR)-N<2-chloro-4,6-dtf octahydro-l,4-methanodipyrido[l,2-a:r,2'-d]pyrazme-9-carboxarnide Step 1 A 5 mL microwave vial was charged with 2-bromo-l-chioro-3,5- difluorobenzene (540 mg, 2.4 mmol), cuprous cyanide (436 mg, 4,87 mmol), tetrakis(triphenylphosphme)palladium (63 mg, 0.05 mmol), sealed, and evacuated/backfilled with nitrogen. To this was added 5 mL degassed DMF. The sealed vessel was heated at 110 C for 18 hours, diluted with ethyl acetate, and washed sequentially with twice 9:1 NH40H:NH4Ci aq twice 5% LiCl(aq ), and brine. The organic phase was then dried over magnesium sulfate, filtered, and concentrated. The crude residue was purified by flash chromatography (100% hexanes) to afford 2-chloro-4,6- difiuorobenzonitrile. - MR (400 MHz, Chloroform-*/) delta 7.13 (dt, J ------- 8.0, 1.9 Hz, 1H), 6.93 (td, J = 8.5, 2.3 Hz, 1H).
The synthetic route of 1020198-58-6 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; GILEAD SCIENCES, INC.; JIN, Haolun; LAZERWITH, Scott, E.; MARTIN, Teresa, Alejandra, Trejo; BACON, Elizabeth, M.; COTTELL, Jeromy, J.; CAI, Zhenhong, R.; PYUN, Hyung-Jung; MORGANELLI, Philip, Anthony; JI, Mingzhe; TAYLOR, James, G.; CHEN, Xiaowu; MISH, Michael, R.; DESAI, Manoj, C.; WO2014/100323; (2014); A1;,
Chloride – Wikipedia,
Chlorides – an overview | ScienceDirect Topics