Related Products of 658-99-1, These common heterocyclic compound, 658-99-1, name is 2-(3,4-Difluorophenyl)acetonitrile, 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.
Methyl (3R,4R)-3-(3-chlorophenyl)-4-cyano-4-(3,4-difluorophenyl)butanoate (Table 1, Example 10) [0772] RRN 13a) Preparation of the diastereomeric methyl 3-(3-chlorophenyl)-4-cyano-4-(3,4-difluorophenyl)butanoates: [0773] Under protective gas (Ar), 0.779 g (5.086 mmol) of (3,4-difluorophenyl)acetonitrile and 0.1 ml of sodium methoxide solution (30% in methanol) were added to 1.000 g (5.086 mmol) of methyl 3-(3-chlorophenyl)acrylate in 12.0 ml of methanol, and the mixture was stirred in a closed vessel in a microwave oven at 100 C. for 4 h. The solvent was removed under reduced pressure, the residue was taken up in dichloromethane and the mixture was washed twice with in each case 25 ml of water. The combined organic phases were dried over sodium sulfate and the solvent was removed under reduced pressure. Chromatography of the residue on silica gel (ethyl acetate/heptane=20:80) gave 0.738 g (37% of theory) of the diastereomeric methyl 3-(3-chlorophenyl)-4-cyano-4-(3,4-difluorophenyl)butanoate (erythro:threo=43:57, comparison of the doublets in the 1H-NMR in CDCl3 at 4.40 and 4.08 ppm).
Statistics shows that 2-(3,4-Difluorophenyl)acetonitrile is playing an increasingly important role. we look forward to future research findings about 658-99-1.
Reference:
Patent; Jakobi, Harald; Mosrin, Marc; Gatzweiler, Elmar; Haeuser-Hahn, Isolde; Heinemann, Ines; Rosinger, Christopher Hugh; Angermann, Alfred; Hoffmann, Michael Gerhard; Schnatterer, Stefan; Zeiss, Hans-Joachim; US2014/194291; (2014); A1;,
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