Extracurricular laboratory: Synthetic route of 437-83-2

The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. We look forward to the emergence of more reaction modes in the future.

Application of 437-83-2, A common heterocyclic compound, 437-83-2, name is 3-Fluoro-2-methoxyaniline, molecular formula is C7H8FNO, 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 1[00180j To a stirred solution of Intermediate 1(0.33 g, 1.61 mmol) in DMA (3 mL) was added 3-fluoro-2-methoxyaniline (0.27 g, 1.9 mmol) followed by NaHMDS (1M in THF, 4.83mL, 4.83 mmol). The reaction was stirred for 30 minutes and then water (30 mL) was gradually added resulting in the product crashing out as a precipitate. The product was collected by filtration, washed with additional water and then dried undervacuum providing Intermediate 15 (476 mg, 95% yield). LC retention time 3.22 mm [A]. MS(Ej m/z: 310 (MHj.

The basis of chemical reaction formula synthesis, the synthesis route is composed of some specific reactions and combined according to certain logical thinking. We look forward to the emergence of more reaction modes in the future.

Reference:
Patent; BRISTOL-MYERS SQUIBB COMPANY; MOSLIN, Ryan M.; LIN, Shuqun; WEINSTEIN, David S.; WROBLESKI, Stephen T.; ZHANG, Yanlei; TOKARSKI, John S.; WO2014/74660; (2014); A1;,
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