Electric Literature of 153248-46-5, A common heterocyclic compound, 153248-46-5, name is [1-[(Boc-amino)methyl]cyclopropyl]methanol, molecular formula is C10H19NO3, 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 solution of PPh3 (242 mg, 0.92 mmol) in anhydrous tetrahydrofuran (10 mL) was added DIAD (186 mg, 0.92 mmol) by syringe at 05 C, followed by a solution of tert-butyl (1-(hydroxymethyl)cyclopropyl)methylcarbamate (110-13) (185 mg, 0.92 mmol) in anhydrous tetrahydrofuran (5 mL). The resulting mixture was poured into a solution of compound 308-3 (100 mg, 0.306 mmol) in anhydrous tetrahydrofuran (5 mL) at ambient temperature and stirred for 1 h. The reaction mixture was quenched with water and extracted with ethyl acetate. The organic layer was washed with water and brine, dried over anhydrous sodium sulfate and evaporated in vacuo. The crude product was purified by column chromatography (dichloromethane/ethyl acetate: 5/1) to afford the title compound 309-13 as a yellow solid (400 mg, crude). LCMS: 510.5 [M+1] .
The synthetic route of 153248-46-5 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; PHARMAENGINE, INC.; CAI, Xiong; QIAN, Changgeng; WANG, Yanong Daniel; (98 pag.)WO2017/132928; (2017); A1;,
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