Application of 239463-85-5, A common heterocyclic compound, 239463-85-5, name is (R)-3-(5-(2-Aminopropyl)-7-cyanoindolin-1-yl)propyl benzoate (2R,3R)-2,3-dihydroxysuccinate, molecular formula is C26H31N3O8, its traditional synthetic route has been very mature, but the traditional synthetic route has various shortcomings, such as complicated route, low yield, poor purity, etc, below Introduce a new synthetic route.
in a container having an inner volume of 5 E and equipped with a reflux condenser, a thermometer, and a stirrer, 317 g (0.62 moles) of 3-{5-[(2R)-2-aminopropyl]-7- cyano-2,3-dihydro-1H-indol-l-yl}propio benzoate.mono(2R,3R)-tartrate, 1.8 E of ethyl acetate, and 1280 g (1.83moles) of a 20% aqueous potassium carbonate solution were mixed and stirred at room temperature for 1 hout10108] After completion of the stirring, an organic phase was separated from the reaction liquid, and the obtained organic phase was concentrated under reduced pressure. The concentrate, 1.8 E of acetonitrile, 69 g (0.65 moles) of sodium carbonate, 10 g (0.03 moles) of tetrabutylammonium bromide, and 233 g (0.74 moles) of 2-[2-(2,2,2-trifluoroeth- oxy)phenoxy]ethyl methanesulfonate were mixed and subjected to reaction under stirring at 75 to 85 C. for 30 hours. 10109] After completion of the reaction, the reaction liquid was cooled to room temperature and then filtered, with the result that 2.2 kg of an acetonitrile solution of 3-(7-cyano- 5-[(2R)-2-({2-[2-(2,2,2-trifluoroethoxy)phenoxy]ethyl}amino)propyl] -2,3-dihydro-l H-indol-l -yl}propylbenzoate (content: 14.2 mass %, 0.53 moles) was obtained (yield: 85%).
The synthetic route of 239463-85-5 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; UBE INDUSTRIES, LTD.; MOTOYAMA, Takahiro; TAKATA, Katsunori; FUKUHARA, Yasuaki; UEMURA, Masato; SADO, Tatsunori; KASAI, Atsuyuki; (20 pag.)US2017/8842; (2017); A1;,
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