Synthetic Route of 77326-36-4, A common heterocyclic compound, 77326-36-4, name is 2-Amino-6-fluorobenzonitrile, molecular formula is C7H5FN2, 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 (R)-1-(3-(hydroxymethyl)piperidin-1-yl)-3-methylbutan-1-one5 (Example 34c) (145 mg, 0.73 mmol) in THF (15 mL) was added NaH (44 mg, 1.09 mmol,60% dispersion in mineral oil) at 0 C. The reaction was warmed to room temperature andstirred for 15 minutes, at which time 2-amino-6-fluorobenzonitrile (109 mg, 0.80 mmol) wasadded. The mixture was heated at 80 C overnight, quenched with water, concentrated underreduced pressure to remove THF and extracted with EtOAc (3X). The combined extracts10 were dried over Na2S04, filtered, concentrated under reduced pressure and purified by flashchromatography on silica gel (EtOAc/hexanes). The residue was further purified by chiralHPLC (normal phase, ethanol/isopropanol/methanol/hexanes) to give the title compound as awhite solid (96 mg, 41% ). MS 316 (MH+).
The synthetic route of 77326-36-4 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; SENOMYX, INC.; TACHDJIAN, Catherine; KARANEWSKY, Donald; WERNER, Sara; DARMOHUSODO, Vincent; YAMAMOTO, Jeff; WO2014/25706; (2014); A1;,
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