With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.373608-48-1,tert-Butyl 4-(3-aminopropyl)piperazine-1-carboxylate,as a common compound, the synthetic route is as follows.
EXAMPLE 17[4-(Benzo[b]thiophen-2-yl)-5-methyl-pyrimidin-2-yl]-[3-(piperazin-1-yl)-propyl]-amine; 4-(3-Aminopropyl)-piperazine-1-carboxylic acid tert-butyl ester (261 mg, 1.07 mmol) is added to a stirred suspension of 4-(benzo[b]thiophen-2-yl)-2-chloro-5-methyl-pyrimidine (140 mg, 0.537 mmol) and diisopropylethylamine (140 muL, 0.805 mmol) in anhydrous 1,4-dioxane (3.5 mL) at ambient temperature under nitrogen. The resultant mixture is heated in an oil bath at 95 C. for 36 hours. At ambient temperature the mixture is concentrated and chromatographed on silica gel, eluting with 2 M NH3/CH3OH in dichloromethane 0-6%, to give 4-{3-[4-(benzo[b]thiophen-2-yl)-5-methyl-pyrimidin-2-yl]-amino-propyl}-piperazine-1-carboxylic acid tert-butyl ester as a white solid (178 mg, 70% yield).TFA (1 mL) is added to a stirred solution of the above product (168 mg, 0.359 mmol) and triethylsilane (0.172 mL, 1.08 mmol) in anhydrous 1,2-dichloroethane (3 mL) at ambient temperature under nitrogen. The resultant solution is allowed to stir for 8 hours. After concentration, the crude product is suspended in CH3OH (5 mL)/dichloromethane (3 mL) then treated with 2.5 N lithium hydroxide (LiOH) (0.43 mL) before it is chromatographed on silica gel, eluting with 2 M NH3/CH3OH in dichloromethane 5-20%, to give the title compound as a yellowish solid (132 mg, 100% yield). ES+(m/z) 368 [M+H]., 373608-48-1
The synthetic route of 373608-48-1 has been constantly updated, and we look forward to future research findings.
Reference£º
Patent; Dahnke, Karl Robert; Lin, Ho-Shen; Richett, Michael Enrico; Shih, Chuan; Wang, Q May; Zhang, Bo; US2008/306082; (2008); A1;,
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