With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.934-98-5,2-(4-Methylpiperazin-1-yl)ethanamine,as a common compound, the synthetic route is as follows.
934-98-5, General method F; A mixture of the appropriate sulfinyl derivative such as Intermediate 39 described hereinbefore (ex:2-methanesulfinyl-5-(3-trifluoromethoxy-phenyl)-imidazo[2, 1 – b][1 ,3,4]thiadiazole) (1 equiv), the appropriate amine (1.5 equiv) (ex: 2-(4-methyl- piperazin-1 -yl)-ethylamine) and Et3N (2 equiv) (0.092 mL, 0.662 mmol) in isopropanol (15 mL/mmol) was heated in a sealed tube at 110 ¡ãC for 40 h. On cooling, DCM was added and the mixture was washed with water. The organic layer was dried (sodium sulfate), filtered and concentrated. The residue was purified by column chromatography (Isolute/Flash, Sill, 0percent to 20percent MeOH in DCM) to give the desired product (ex: [2-(4-methyl-piperazin-1 -yl)-ethyl]-[5-(3- trifluoromethoxy-phenyl)-imidazo[2,1-b][1 ,3,4]thiadiazol-2-yl]-amine).; Example 47; [2-(4- ethyl-piperazin-1-yl)-ethyl]-[5-(3-trifluoromethoxy-phenyl)- imidazo[2,1-b][1,3,4]t iadiazol-2-yl]-amine; HPLC-MS (method 1): Rt= 3.15 min, [M+1]+ m/z 427.2.1H NMR (300 MHz, MeOD) delta 7.99 (s, 1 H), 7.85 (d, J = 8.0 Hz, 1 H), 7.48 (s, 1 H), 7.46 (t, J = 8.1 Hz, 1 H), 7.15 (d, J = 8.2 Hz, 1 H), 3.57 (t, J = 6.5 Hz, 2H), 2.69 (t, J = 6.5 Hz, 2H), 2.60 (m, 4H), 2.50 (m, 4H), 2.27 (s, 3H).Yield: 48percent
934-98-5 2-(4-Methylpiperazin-1-yl)ethanamine 70284, apiperazines compound, is more and more widely used in various fields.
Reference£º
Patent; CENTRO NACIONAL DE INVESTIGACIONES ONCOLOGICAS (CNIO); PASTOR FERNANDEZ, Joaquin; GARCIA COLLAZO, Ana, Maria; NOYA MARINO, Beatriz; GONZALEZ CANTALAPIEDRA, Esther; WO2012/20217; (2012); A1;,
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