13220-46-7, name is 4-Methylindolin-2-one, belongs to indolines-derivatives compound, is considered to be a conventional heterocyclic compound, which is widely used in drug synthesis. The chemical synthesis route is as follows. Safety of 4-Methylindolin-2-one
(S)-5-(2-Hydroxy-3-morpholin-4-yl-propyl)-3-methyl-4-oxo-1,4,5,6,7,8-hexahydro-pyrrolo[3,2-c]azepine-2-carbaldehyde 78f (40 mg, 0.12 mmol 1) and 4-methyl-1,3-dihydro-indol-2-one (18 mg, 0.12 mmol) were dissolved in 1.5 ml of ethanol, and added with 6mul of piperidine to the solution at room temperature. Upon completion of the addition, the reaction mixture was stirred at 45C for 16 hours. After thin lay chromatography showed the disappearance of starting materials, the reaction mixture was naturally cooled down to room temperature, and filtered. The filter cake was washed with anhydrous ethanol (1 ml¡Á2) and dried to obtain the title compound (S,Z)-5-(2-hydroxy-3-morpholinopropyl)-3-methyl-2-((4-methyl-2-oxoindolin-3-ylide ne)methyl)-5,6,7,8-tetrahydropyrrolo[3,2-c]azepin-4(1H)-one 83 (35 mg, yield 63.6%) as a yellow solid. MSm/z(ESI): 465.2(M+1) 1NMR(400 MHz, DMSO-d6) delta13.715(s, 1H, pyrrole-NH),10.934(s, 1H, indole-NH),7.572(s, 1H, -CH=C), 7.057 (t, 1H, -ArH), 6.840?6.821(d, 1H, -ArH), 6.790?6.771(d, 1H, -ArH), 4.737?4.725(d, 1H, -OH), 3.92(m, 1H, -CHOH), 3.75 (dd, 1H, seven-membered ring intra amide -NCH2), 3.58(t, 4H, morpholin2¡Á-CH2O), 3.441 (m, 2H, seven-membered ring -NCH2), 3.15(m, 1H, seven-membered ring outer amide-NCH2), 2.939(t, 2H, -CH2CH=C), 2.594(s, 3H, pyrrole-CH3), 2.426 (m, 4H, morpholin intra 2¡Á-CH2N), 2.388(s, 3H, pyrrole-CH3), 2.309?2.293(m, 2H, morpholin outer-NCH2), 2.078(m, 2H, seven-membered ring CH2-CH2-CH2)
The synthetic route of 13220-46-7 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; Shanghai Hengrui Pharmaceutical Co. Ltd.; EP2157093; (2010); A1;,
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