Analyzing the synthesis route of 154590-35-9

The synthetic route of 154590-35-9 has been constantly updated, and we look forward to future research findings.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.154590-35-9,tert-Butyl 4-(4-amino-2-fluorophenyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.,154590-35-9

To a solution of 4-(4-Amino-2-fluoro-phenyl)-piperazine-1 -carboxylic acid te/t-butyl ester (0.50 g, 1.7 mmol) and (0.38 g, 1.9 mmol) in CH2CI2 (30 ml_) was added 1 -hydroxybenzotriazole hydrate (0.27 g, 2.0 mmol), and 1 -[3-(dimethylamino)propyl]-3-ethylcarbodiimide hydrochloride (0.38 g, 2.0 mmol). After stirring at room temperature for 18 h, the reaction was diluted with 1 N NaOH (50 ml_) and extracted with CH2CI2 (3×50 ml_). The organic extracts were combined, dried (Na2SO4), and concentrated. Chromatography of the resulting residue (SiO2: EtOAc/hexanes) yielded 4-{4- [(biphenyl-2-carbonyl)-amino]-2-fluoro-phenyl}-piperazine-1 -carboxylic acid tert- butyl ester, which was further dissolved in MeOH (20 ml_) and 4N HCI in dioxanes. After stirring for 5 h, the reaction mixture was concentrated down, neutralized with 1 N NaOH, and extracted with EtOAc (3x75ml_). The orgranic extracts were combined, dried (Na2SO4), and the solvent was evaporated under reduced pressure to yield the title compound.MS (ESI): mass calcd. for 023Hz2FN3O, 375.17; m/z found, 376.3 [IvRH]+.

The synthetic route of 154590-35-9 has been constantly updated, and we look forward to future research findings.

Reference£º
Patent; JANSSEN PHARMACEUTICA, N.V.; WO2009/6185; (2009); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics