With the rapid development and complex challenges of chemical substances, new drug synthesis pathways are usually the most effective.1059630-08-8,(4aS,9bR)-Ethyl 6-bromo-3,4,4a,5-tetrahydro-1H-pyrido[4,3-b]indole-2(9bH)-carboxylate,as a common compound, the synthetic route is as follows.
To a degassed mixture of (4aS,9bR)-ethyl 6-bromo-3,4,4a,5- tetrahydro-lH-pyrido[4,3-b]indole-2(9bH)-carboxylate (1.60 g, 8.0 mmol), 2-chloro-2,2- dideuterio-N-methylacetamide (1.74 g, 16 mmol), and KI (2.68 g, l6mmol) in dioxane (28 mL), diisopropylethylamine (2.8 mL, 16 mmol) is added at room temperature. The reaction mixture is then heated to 104 C under vigorous stirring for 20 h. Solvents are removed under vacuum and the residue is suspended in dichloromethane (50 mL) and extracted with water (20 mL). The organic phase is separated, dried over K2CO3 and concentrated to a residue. (0256) The product is purified by silica gel column chromatography using a gradient of 0 – 100% mixed solvents [ethyl acetate/methanol (10 : 1 v/v) ] in ethyl acetate to yield (4aS,9bR)-ethyl 6-bromo-5-(l,l-dideuterio-2-(methylamino)-2-oxoethyl)-3,4,4a,5-tetrahydro-lH-pyrido[4,3- b]indole-2(9bH)-carboxylate a brown solid (1.15 g, yield 36%). MS (ESI) m/z 398.1 [M+l] +.
1059630-08-8, As the paragraph descriping shows that 1059630-08-8 is playing an increasingly important role.
Reference：
Patent; INTRA-CELLULAR THERAPIES, INC.; LI, Peng; DAVIS, Robert; (46 pag.)WO2019/183546; (2019); A1;,
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