Synthetic Route of 130473-26-6, In the chemical reaction process,reaction time,type of solvent,can easily affect the result of the reaction, thereby determining the yield and properties of the reaction product.An updated downstream synthesis route of 130473-26-6 as follows.
C174 (500 mg, 3.42 mmol) is dissolved in 1.5 mL formic acid. The solution is cooled in an ice bath, 30% aqueous hydrogen peroxide (722 muL, 6.8 mmol) is added drop-wise, and the reaction is stirred 1 h in an ice bath, and allowed to stand overnight at 5 C. The mixture is diluted with H2O, the solid is collected, washed with H2O and is dried to give 522 mg of an off-white solid. The formate salt is added to 7 mL H2O, 3 mL 2N NaOH is added, and the pH is adjusted to 3 with 5% aqueous HCl. The precipitate is collected and is dried to afford 1H-pyrrolo[2,3-c]pyridine-5-carboxylic acid (C176) (67% yield). HRMS (FAB) calculated for C8H6N2O2+H: 163.0508, found 163.0507 (M+H). Example 23(i) can be obtained by coupling either exo-[2.2.1]-3-Amine or endo-[2.2.1]-3-Amine with C176.
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,130473-26-6, its application will become more common.
Reference:
Patent; Walker, Daniel Patrick; Piotrowski, David W.; Jacobsen, Eric Jon; Acker, Brad A.; Wishka, Donn G.; Reitz, Steven Charles; Groppi JR., Vincent E.; US2003/153595; (2003); A1;,
Pyridine – Wikipedia,
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