Analyzing the synthesis route of 618910-07-9

618910-07-9 8-Methoxy-5-methyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole 24206808, aindole-building-block compound, is more and more widely used in various fields.

With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.618910-07-9,8-Methoxy-5-methyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole,as a common compound, the synthetic route is as follows.

General procedure: To degassed tetrahydrofuran (5 mL) was added chloro-(2-dicyclohexylphosphino-2′,6′-diisopropoxy-1 ,1 ‘-biphenyl)[2-(2-aminoethyl)phenyl]palladium(ll)-methyl-f-butyl ether adduct (PdRuPhos G1 ) (0.017 g, 0.024 mmol), 2-dicyclohexylphosphino-2?,6’-diisopropoxybiphenyl (RuPho) (0.011 g, 0.024 mmol), the title compound from Preparative Example 2 (0.05 g, 0.024 mmol), and the commercially available 4-(6-bromobenzo[d]thiazol-2-yl)morpholine (0.073 g, 0.029 mmol). Then, a 1 M solution of lithium bis(trimethylsilyl)amide (LiHMDS) in tetrahydrofuran (1 mL, 1 mmol) was added. The resulting reaction mixture was heated at reflux for 2 hours. The reaction mixture was cooled to room temperature, dissolved in dichloromethane (100 mL). The organic phase was washed with water and brine and dried over Na2S04. The solvent was removed under reduced pressure. The crude product was purified on a silica gel column using a Biotage Isolera One purification system employing an ethyl acetate/n-heptane gradient (80/20 => 100/0) to afford the title compound (0.070 g, 69 %)., 618910-07-9

618910-07-9 8-Methoxy-5-methyl-2,3,4,5-tetrahydro-1H-pyrido[4,3-b]indole 24206808, aindole-building-block compound, is more and more widely used in various fields.

Reference£º
Patent; AC IMMUNE SA; NAMPALLY, Sreenivasachary; GABELLIERI, Emanuele; MOLETTE, Jerome; (220 pag.)WO2019/134978; (2019); A1;,
Indole alkaloid derivatives as building blocks of natural products from?Bacillus thuringiensis?and?Bacillus velezensis?and their antibacterial and antifungal activity study
Preparation of Indole Containing Building Blocks for the Regiospecific Construction of Indole Appended Pyrazoles and Pyrroles