Application of 198989-07-0, A common heterocyclic compound, 198989-07-0, name is tert-Butyl 2,5-diazabicyclo[2.2.1]heptane-2-carboxylate, molecular formula is C10H18N2O2, 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.
Step 2.4: To a solution of 1?-(5-(4-acetamidopyridin-2-yl)pyrimidin-2-yl)spiro[cyclopropane-1 ,3?-indoline]- 6?-carboxylic acid (0.25 g, 0.62 mmol, 1 eq) in DMF (5 mL), the TBTU (0.24 g, 0.747 mmol, 1.2 eq), NMM (0.126 g, 1.25 mmoL, 2 eq) and 2,5-diaza-bicyclo[2.2.1]heptane-2-carboxylic acid tert-butyl ester (0.123 g, 0.623 mmol, 1 eq) were added at RT. RM was then stirred at RT for 16 h. After completion of reaction,reaction mixture was quenched with ice water (40 mL) and a solid was precipitated out. The solid was filtered off and re-dissolved in EtOAc (50 mL). The EtOAc solution of the desired compound was washed with water (2 x 40 mL), brine (40 mL), dried over Na2SO4, filtered and evaporated under reduced pressure to get the crude product. The crude product was triturated with Et20-hexane (3 x) to afford tert-butyl 5-(1 (5-(4-acetamidopyridin-2-yl)pyrimidin-2-yl)spiro[cyclopropane-1 ,3-indolinj-6?-ylcarbonyl)-2,5-diazabicycle-[2.2.1]heptane-2-carboxylate (0.35 g, 96.9%) as white solid.
The synthetic route of 198989-07-0 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; GRUeNENTHAL GMBH; NARDI, Antonio; JAKOB, Florian; KONETZKI, Ingo; CRAAN, Tobias; HESSLINGER, Christian; DOODEMAN, Robin; (0 pag.)WO2016/8593; (2016); A1;,
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