Application of 201940-08-1,Some common heterocyclic compound, 201940-08-1, name is tert-Butyl 5-bromoisoindoline-2-carboxylate, molecular formula is C13H16BrNO2, 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.
Under nitrogen protection,A solution of 5-bromo-2- (tert-butoxycarbonyl) isoindoline (1.2 g, 4 mmol)And boronic acid pinacol ester (2 g, 8 mmol)Was dissolved in dimethylsulfoxide (20 mL)To this was added potassium acetate (1.6 g, 16 mmol) andPd (dppf) Cl2CH2Cl2 (327 mg, 0.4 mmol).The reaction solution was heated and stirred at 90 C for 12 hours,Cool to room temperature and pour into acetic acidEthyl acetate / water (300 mL / 100 mL), the separated organic phase was washed with brine (100 mL), dried over anhydrous sodium sulfate,Filtered and concentrated under reduced pressure. The residue was purified by silica gel column chromatography (petroleum ether / ethyl acetate (v / v) = 20/1)The title compound was obtained as a yellow oil (1 g, 73%).
The synthetic route of 201940-08-1 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; Guangdong Dongyangguang Pharmaceutical Co., Ltd.; Jiatuo Sciences Corporation; Xi Ning; Wang Ruyong; Wang Liang; (112 pag.)CN104016979; (2017); B;,
Indoline – Wikipedia,
Indoline | C8H9N – PubChem