With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.13484-40-7,1-(2-Methoxyethyl)piperazine,as a common compound, the synthetic route is as follows.
EXAMPLE 11; Preparation of (N-(2-aminophenyl)-4-{3-methyl-5-[(4-(2-methoxyethyl)-piperazin-1-yl)methyl]pyridin-2-yl}benzamide); tert-Butyl (2-{[4-(5-formylpyridin-2-yl)benzoyl]amino}phenyl)carbamate (0.20 g, 0.4634 mmol; prepared as described in method 3), 1-(2-methoxyethyl)-piperazine (104 mg, 0.7 mmol) and acetic acid (27 mul, 0.4634 mmol) were dissolved in tetrahydrofuran (5 ml). The mixture was stirred at ambient temperature for 1 hour then sodium triacetoxyborohydride (147 mg, 0.695 mmol) added and the mixture stirred for a further 16 hours. The mixture was concentrated and partitioned between dichloromethane (5 ml) and saturated sodium bicarbonate (5 ml). The organics were washed with further saturated sodium bicarbonate (2¡Á5 ml) and brine (5 ml) then dried over magnesium sulphate and filtered. This solution was then treated with trifluoroacetic acid (1.0 ml) and the solution then stirred at ambient temperature for 2 hours. The resulting solution was absorbed onto an SCX-2 column, which was washed with methanol (3 column volumes) and the product eluted with a 2M solution of ammonia in methanol (3 column volumes) which was concentrated to give the product as a gum. The residue was purified by acid modified reverse phase HPLC. Fractions containing the product were absorbed onto an SCX-2 column and washed with methanol (2 column volumes) then the products eluted with a 2M solution of ammonia in methanol (2 column volumes) and concentrated under reduced pressure, to give a residue which was triturated with ether to give title compound as a solid (12 mg, 6%). NMR Spectrum: (DMSO-d6); 2.37 (s, 3H), 2.43 (m, 10H), 3.24 (s, 3H), 3.43 (t, 2H), 3.53 (s, 2H), 4.92 (s, 2H), 6.62 (m, 1H), 6.80 (m, 1H), 6.99 (m, 1H), 7.21 (m, 1H), 7.66 (s, 1H), 7.69 (d, 2H), 8.07 (d, 2H), 8.42 (m, 1H), 9.72 (s, 1H). Mass Spectrum: M+H+460., 13484-40-7
13484-40-7 1-(2-Methoxyethyl)piperazine 2734638, apiperazines compound, is more and more widely used in various fields.
Reference£º
Patent; ASTRAZENECA AB; US2008/119451; (2008); A1;,
Piperazine – Wikipedia
Piperazines – an overview | ScienceDirect Topics