Synthetic Route of 102359-00-2, These common heterocyclic compound, 102359-00-2, name is 2-Oxoindoline-5-carboxylic Acid, 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 2-oxoindoline-5-carboxylic acid (0.177 g, 1.00 mmol) in DMF (2 mL), were added EDCI.HCl (0.24 g, 1.25 mmol), HOBt (0.168 g, 1.25 mmol) and triethylamine (0.35 mL, 2.5 mmol). The solution was stirred for 10 min at 0oC. tert- Butyl ((2S)-1-(4-(1-aminoethyl)piperidin-1-yl)-1-oxopropan-2-yl)carbamate (0.25 g, 0.83 mmol) was added and the reaction stirred at rt for 6 h. The progress of the reaction was monitored by TLC. After complete consumption of starting material, the reaction was quenched with water and extracted with ethyl acetate. The organic layer was separated, washed with brine, dried over anhydrous Na2SO4and concentrated under reduced pressure to obtain a crude residue which was purified by column chromatography to afford tert-butyl ((2S)-1-oxo-1-(4-(1-(2-oxoindoline-5-carboxamido)ethyl)piperidin-1- yl)propan-2-yl)carbamate (0.11 g, 28%)
The synthetic route of 102359-00-2 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; Epizyme, Inc.; Poley, Megan Allen Clunan; Kunz, Kevin Wayne; Mills, James Edward John; Mitchell, Lona Helen; munckhof, Michael John; Harvey, Darren Martin; (303 pag.)KR2017/45749; (2017); A;,
Indoline – Wikipedia,
Indoline | C8H9N – PubChem