With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.162046-66-4,4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid,as a common compound, the synthetic route is as follows.
Example 36 Preparation of N -(8-fluoro-2-methylimidazo[1,2-a]pyridin-6-yl)-4-(piperazin-1-yl) benzamide hydrochloride To a solution of 4-(4-(tert-butoxycarbonyl)piperazin-1-yl)benzoic acid (commercial) (109 mg,357 flmol) in N,N-dimethylformamide (1.00 ml) under nitrogen at room temperature, wereadded HA TU ( 0-(7-azabenzotriazol-1-yl)-N ,N ,N’ ,N’-tetramethyluronium hexafluorophosphate)(204 mg, 536 flmol) and N-ethyldiisopropylamine (185 mg, 243 f..Ll, 1.43 mmol). After 5 minutesstirring at room temperature, 8-fluoro-2-methyl-imidazo[1,2-a]pyridin-6-ylamine hydrochloride (Example B.4) (72 mg, 357 flmol) was added. The mixture was stirred at room temperature for21 hours and then at 60C for 2 hours. The solvent was removed in vacuo. The residue was taken in a saturated aqueous solution of bicarbonate and extracted three times with ethyl acetate. The combined extracts were dried over sodium sulfate, filtered and concentrated in vacuo. The crude oil was purified on silica gel (Eluent: heptane/ethyl acetate 0 to 10%) to provide 78 mg of tert-butyl 4-(4-(8-fluoro-2-methylimidazo[1,2-a]pyridin-6-ylcarbamoyl)phenyl)piperazine-1-carboxylate. To a suspension of this compound (40 mg, 88.2 flmol) in methanol (400 f..Ll) was added HC14M in dioxane (221 f..Ll, 882 flmol). The light yellow suspension was stirred at roomtemperature for 17 hours. The solid was filtered, washed with ether and hexane and dried toprovide 25 mg (72.7 %) of the title compound as a light yellow solid., 162046-66-4
162046-66-4 4-(4-(tert-Butoxycarbonyl)piperazin-1-yl)benzoic acid 2795508, apiperazines compound, is more and more widely used in various fields.
Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; PTC THERAPEUTICS INC.; DAKKA, Amal; GREEN, Luke; KARP, Gary; NARASIMHAN, Jana; NARYSHKIN, Nikolai; PINARD, Emmanuel; QI, Hongyan; RATNI, Hasane; RISHER, Nicole; WEETALL, Marla; WOLL, Matthew; WO2014/209841; (2014); A2;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics