With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.132710-90-8,1-Boc-4-(3-hydroxypropyl)piperazine,as a common compound, the synthetic route is as follows.
To 0.5 g (2.05 mmol) of tert-butyl 4-(3-hydroxypropyl)piperazine-1-carboxylate, 0.3 g (2.46 mmol) of 4-hydroxybenzaldehyde and 1 g (3.07 mmol) of resin-supported triphenyl-phosphine (3 mmol/g of resin) diluted in 14.5 ml of anhydrous tetrahydrofuran, is added dropwise at 0C under argon 0.614 ml (3.07 mmol) of diisopropyldiazene-1,2-dicarboxylate. The reaction mixture is stirred at room temperature for 20h. The solid is filtered then rinsed in dichloromethane. The filtrate is concentrated and diluted in a sodium hydroxide solution (1M) and the product is extracted several times with ethyl acetate. The organic phases are combined, dried over magnesium sulfate, and concentrated. The residue is purified by chromatography on silica (cyclohexane/ethyl acetate eluent: 4:6 to 100% ethyl acetate) to yield 0.58 g of tert-butyl 4-(3-(4-formylphenoxy)propyl)piperazine-l-carboxylate in the form of a colourless oil.LCMS (ESI, m/z): (M+l) 348.91H-NMR: deltaEta pm 400 MHz, DMSO: 9.87 (1H, s, CHO), 7.86 (2H, d, CH^), 7.12 (2H, d, CHaro , 4.13 (2H, t, CH2), 3.28-3.31 (4H, m, 2CH2), 2.44 (2H, t, CH2),2.31-2.34 (4H, m, 2CH2), 1.91 (2H, q, CH2), 1.40 (9H, s, 3CH3).
132710-90-8, As the paragraph descriping shows that 132710-90-8 is playing an increasingly important role.
Reference£º
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;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics