With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.70261-82-4,4-(4-Methylpiperazin-1-ylmethyl)phenylamine,as a common compound, the synthetic route is as follows.
To a degassed solution of N-(4-(2-chloro-4-(2-methoxyethoxy)-7-((2-(trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl)phenyl)-2,5-difluorobenzene sulfonamide (140 mg, 0.224 mmol in l,4-dioxane) was added 4-((4-methylpiperazin-l- yl)methyl)aniline (51 mg, 0.246 mmol), palladium(II) acetate (1 mg, 0.004 mmol), SPhos (3 mg, 0.008 mmol) and cesium carbonate (146 mg, 0.448 mmol). The mixture was heated under microwave irradiation at 150W for 20 min. The organic solvent was removed under vacuum and the aqueous layer was extracted with ethyl acetate. The combined organic layers were washed with brine, dried over anhydrous sodium sulfate, and filtered. The filtrate was evaporated under reduced pressure. The product was purified by silica gel column chromatography using dichloro methane and methanol gradient eluents to give 2,5-difluoro- N-(4-(4-(2-methoxyethoxy)-2-((4-((4-methylpiperazin-l-yl)methyl)phenyl)amino)-7-((2- (trimethylsilyl)ethoxy)methyl)-7H-pyrrolo[2,3-d]pyrimidin-5-yl)phenyl)benzenesulfonamide in 41% yield as a pale yellow solid. NMR (500 MHz, CDCh): d 7.63 (d, J = 8.5 Hz, 2H), 7.61 (d, J = 8.3 Hz, 2H), 7.53-7.57 (m, 1H), 7.25 (d, J = 8.3 Hz, 2H), 7.14-7.21 (m, 2H), 7.11 (d, J = 8.5 Hz, 2H), 6.96 (s, 2H), 5.51 (s, 2H), 4.55 (t, J = 4.6 Hz, 2H), 3.69 (t, J = 4.6 Hz, 2H), 3.56 (t, J = 8.3 Hz, 2H), 3.47 (s, 2H), 3.37(s, 3H), 2.48 (br, 8H), 2.29 (s, 3H), 0.92 (t, J = 8.3 Hz, 2H), -0.09 (s, 9H); Mass (ESI) m/z 794.58, 397.79 [M+H+], 70261-82-4
The synthetic route of 70261-82-4 has been constantly updated, and we look forward to future research findings.
Reference：
Patent; DEVELOPMENT CENTER FOR BIOTECHNOLOGY; DCB-USA LLC; YEN, Shih-Chieh; LIAO, Chu-Bin; WANG, Hui-Chen; CHEN, Po-Ting; PAN, Yu-Chih; LI, Tsung-Hui; CHEN, Bo-Rong; CHIOU, Shian-Yi; (64 pag.)WO2019/133629; (2019); A1;,
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