With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.31166-44-6,1-Cbz-Piperazine,as a common compound, the synthetic route is as follows.
N-(4-Bromophenyl)-4-methoxybenzamide (2 g, 6.53 mmol), Cbz-piperazine (1.38 g, 7.18 mmol), XPhos (623 mg, 1.31 mmol) and NaO/Bu (1.38 g, 14.4 mmol) were suspended in dioxane (20 ml) and degassed with nitrogen for 30 minutes. [Pd2(dba)3] (598 mg, 0.65 mmol) was then added and the reaction mixture was heated to 90 C for 2 h under N2. The re action was allowed to cool to rt and diluted with H20. The precipitate formed was collected by filtration and washed with H20. The dry residue (3.7 g) was triturated with diethyl ether to afford the title compound (2.85 g, 98%) as a brown solid. NMR (400 MHz, DMSO): d 9.92 (s, 1H), 7.94 (d, J=8.9 Hz, 2H), 7.62 (d, J=9.2 Hz, 2H), 7.40 (d, J=4.5 Hz, 4H), 7.38 – 7.31 (m, 1H), 7.05 (d, J=8.9 Hz, 2H), 6.95 (d, J=9.2 Hz, 2H), 5.12 (s, 2H), 3.84 (s, 3H), 3.59 – 3.56 (m, 4H), 3.09 (dd, J=5.0, 5.0 Hz, 4H). LC-MS: Rt = 1.69 min, m/z = 446, [M+H]+.
31166-44-6, 31166-44-6 1-Cbz-Piperazine 643495, apiperazines compound, is more and more widely used in various fields.
Reference£º
Patent; F. HOFFMANN-LA ROCHE AG; HOFFMANN-LA ROCHE INC.; BORRONI, Edilio; GOBBI, Luca; HONER, Michael; EDELMANN, Martin; MITCHELL, Dale; HARDICK, David; SCHMIDT, Wolfgang; STEELE, Christopher; MULLA, Mushtaq; (151 pag.)WO2019/121661; (2019); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics