With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.197638-83-8,1-Boc-4-(4-Formylphenyl)piperazine,as a common compound, the synthetic route is as follows.
To a solution of hydrazine hydrate diluted in 16 ml of dimethylsulf oxide under argon are added dropwise a solution of 4.76 g (16.41 mmol) of tert-butyl 4-(4- formylphenyl)piperazine-l-carboxylate dissolved in 32 ml of dimethylsulfoxide. The reaction mixture is stirred at room temperature for 3h before being cooled over an ice bath. Then, the successive addition is made of 11.45 ml (82 mmol) of triethylamine, 162 mg of copper (I) chloride and, in 5 min, a solution of 8.23 ml (82 mmol) of trichloroacetonitrile diluted in 16 ml of dimethylsulfoxide. The reaction mixture is stirred at room temperature for 18h then poured onto an aqueous 0.1N hydrochloric acid solution. The product is extracted several times with dichloromethane. The organic phases are combined, dried over magnesium sulfate, and concentrated. The residue is purified by chromatography on silica (cyclohexane/ethyl acetate eluent: 8:2) to yield 1.52 g (26%) of tert-butyl 4-(4-(2-chloro-2-cyanovinyl)phenyl)piperazine-l- carboxylate in the form of a yellow solid (mixture of the two isomers Z/E).1H-NMR: deltaEta pm 400 MHz, CDC13:7.70 (2H, d, Cl ), 7.18 (1H, s, CH^), 6.87 (2H, d, CH^), 3.51-3.45 (4H, 2 x CH2), 3.35-3.25 (4H, m, 2 x CH2), 1.49 (9H, s C(CH3)3). (33%)7.62 (2H, d, CH^), 7.21 (1H, s, CH^), 6.87 (2H, d, CH^), 3.51-3.45 (4H, 2 x CH2 -3.25 (4H, m, 2 x CH2), 1.49 (9H, s, C(CH3)3). (66%).
197638-83-8, The synthetic route of 197638-83-8 has been constantly updated, and we look forward to future research findings.
Reference：
Patent; PIERRE FABRE MEDICAMENT; BEDJEGUELAL, Karim; RABOT, Remi; KALOUN, El Bachir; MAYER, Patrice; MARCHAND, Arnaud; RAHIER, Nicolas; SCHAMBEL, Philippe; BIENAYME, Hugues; WO2011/45344; (2011); A1;,
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