With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.216144-45-5,4-(4-Methylpiperazin-1-yl)benzylamine,as a common compound, the synthetic route is as follows.
Stage 3: 6-[4-(4-methylpiperazin-1-yl)benzyl]-5H-quinazolino[3,2-a]quinazoline-5,12(61)-dione hydrochlorideA solution of methyl 2-(2-chloro-4-oxoquinazolin-3(4H)-yl)benzoate (170 mg) and [4-(4-methylpiperazin-1-yl)benzyl]amine (200 mg) in a THF/DCM/Et3N mixture (1 mL/1 mL/1 mL) is stirred for 4 days at ambient temperature then water and dichloromethane are added. After decantation and extractions, the combined organic phases are washed with salt water, dried over Na2SO4 then concentrated under reduced pressure at 40 C. Purification by flash chromatography on silica gel (eluent: dichloromethane/methanol 100:0 to 92:8) produces the expected compound in the form of the free base. The corresponding hydrochloride salt is formed by adding a 1N HCl solution in ethyl ether to the solution of the free base in ethyl acetate. The precipitate obtained is filtered and dried in order to produce the expected hydrochloride compound (85 mg, 36% yield from Stage 2).MS/LC: calculated MM=431.2; m/z=432.3 (MH+)NMR (1H, 400 MHz, DMSO-d6): delta2.83 (d, 3H), 3.12 (m, 4H), 3.48 (d, 2H), 3.81 (d, 2H), 5.55 (s, 2H), 6.98 (AB, 2H), 7.55 (m, 3H), 7.66 (m, 2H), 7.90 (m, 2H), 8.25 (AB, 1H), 8.31 (AB, 1H), 9.11 (AB, 1H), 10.75 (s, 1H)., 216144-45-5
216144-45-5 4-(4-Methylpiperazin-1-yl)benzylamine 2776493, apiperazines compound, is more and more widely used in various fields.
Reference£º
Patent; SOCIETE DE CONSEILS DE RECHERCHES ET D’APPLICATIONS SCIENTIFIQUES (S.C.R.A.S.); US2010/144714; (2010); A1;,
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