1H-Benzimidazole-2-acetonitrile,4-methoxy-(9CI) synthesis

Yield:317817-41-7 75%

Reaction Conditions:

in 5,5-dimethyl-1,3-cyclohexadiene; for 15 h;Reflux;Molecular sieve;

Steps:

4.1.28. 2-(4-(1-Amino-2,4-dicyano-6-methylbenzo[4,5]imidazo[1,2-a]pyridin-3-yl)phenoxy)acetamide (31)

General procedure: A solution of 3-methylbenzene-1,2-diamine (58) (1.50 g, 12.28 mmol) and cyanoacetamide (2.06 g, 24.56 mmol) in xylene (25 ml) was heated under reflux for 15 h in the presence of 4 ? molecular sieves. The hot solvent was decanted and the residue was extracted with Et₂O/MeOH and filtrated. The filtrate was evaporated to dryness.

References:

Lyons, Dani M.;Huttunen, Kristiina M.;Browne, Kylie A.;Ciccone, Annette;Trapani, Joseph A.;Denny, William A.;Spicer, Julie A. [Bioorganic and Medicinal Chemistry,2011,vol. 19,# 13,p. 4091 - 4100] Location in patent:experimental part