Application of 2927-71-1 ,Some common heterocyclic compound, 2927-71-1, molecular formula is C4HCl2FN2, 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.
To a stirred solution of (S)-tert-butyl 3-aminopiperidine-1-carboxylate (1) (1.437 g, 7.18 mmol) in DMF (10 mL) was added DIPEA (1.56 mL, 8.98 mmol) and 2,4-dichloro-5- fluoropyrimidine (2) (1.0 g, 5.98 mmol) in DMF (2 mL) at 0 C drop wise. The reaction mixture was allowed to stir at room temperature for 16 h. After consumption of starting material by TLC (absence of compd-2), the mixture was diluted with ether (75 mL) and washed with ice cold water (3 x 50 mL), brine solution (25 mL), dried over sodium sulfate and concentrated under reduced pressure to afford tert-butyl (S)-3-((2-chloro-5- fluoropyrimidin-4-yl)amino)piperidine-1-carboxylate (3) (1.670 g, 5.06 mmol, 84 % yield) as white solid. TLC system: 30% EA in pet Ether Rf: 0.5 LCMS (ESI): m/z 331.44 (M+1)+
These compound has a wide range of applications. It is believed that with the continuous development of the source of the synthetic route,2927-71-1, its application will become more common.
Reference:
Patent; COCRYSTAL PHARMA, INC.; JACOBSON, Irina, C.; LEE, Sam SK; FEESE, Michael, David; (206 pag.)WO2020/23813; (2020); A1;,
Pyrimidine | C4H4N2 – PubChem,
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