Electric Literature of 56043-01-7, These common heterocyclic compound, 56043-01-7, name is 2-Amino-6-methylbenzonitrile, 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.
A mixture of 6-chloro-N-(4-fluoro-benzyl)-4-isopropyl-nicotinamide (Description 6) (100 mg), 2- amino-6-methyl-benzonitrile (43 mg), cesium carbonate (168mg), tris (dibenzylideneacetone) dipalladium (0) (ex-Aldrich, 3.36mg) and 4,5-bis (diphenylphosphino) – 9,9-dimethylxanthene (ex-Aldrich, 2.3 mg) and 1,4-dioxan (1 ml) was heated to relux under nitrogen for 24h. When cool, the mixture was diluted with ethyl acetate and filtered through a PTFE disc (1.0 M) disc and the filtrate evaporated. The residue was purified using the Biotage Horizon HPFC System and the resultant product was triturated with ether, washed with ether, and dried in vacuo at 40 to give 6- (2-cyano-3-methyl-phenylamino)-N-(4-fluoro-benzyl)-4-isopropyl- nicotinamide (15mg). NMR (d6-DMSO) 8 1.16 (6H, d), 2.46 (3H, s), 3.35-3. 45 (1H, m), 4. 36-4. 47 (2H, m), 6.95 (1H, s), 7.08 (1H, d), 7.13 (1H, t), 7. 35 (2H, m), 7. 39 (2H, t), 7.68 (1H, d), 8.07 (1H, s), 8.9 (1H, m), 9.14 (1H, s). LC/MS t = 3. 27min, [MH+] 403 consistent with molecular formula C24H23FN40
The synthetic route of 56043-01-7 has been constantly updated, and we look forward to future research findings.
Reference:
Patent; GLAXO GROUP LIMITED; DOUGHTY, Jennifer, Margaret; WO2005/74939; (2005); A1;,
Nitrile – Wikipedia,
Nitriles – Chemistry LibreTexts