116599-29-2

Upstream product

• 150-78-7 1,4-dimethoxybezene 
• 6945-76-2 1,4-dimethoxy-2,3-dinitrobenzene 

Downstream Products

• 7711-50-4 4,7-dimethoxybenzimidazole 
• 1075744-30-7 (1R,2R,4R)-2-(2-((3-(4,7-dimethoxy-1H-benzo[d]imidazol-2-yl)propyl)(methyl)amino)ethyl)-5-phenylbicyclo[2.2.2]oct-5-en-2-ol 
• 99922-32-4 4,7-Dimethoxy-2-methyl-1H-benzimidazole 
• 797758-63-5 1,2-dibenzyl-4,7-dimethoxy-1H-benzoimidazole 
• 797758-51-1 1-benzyl-4,7-dimethoxy-2-methyl-1H-benzoimidazole 
• 807317-35-7 1-benzyl-4,7-dihydroxy-1H-benzimidazole 
• 457050-40-7 1-benzyl-1H-benzimidazole-4,7-dione 
• 36098-02-9 1-benzyl-4,7-dimethoxy-1H-benzimidazole 
• 457050-37-2 2-benzyl-4,7-dimethoxy-1H-benzoimidazole 
• 89427-14-5 4,7-dimethoxy-2-trifluoromethyl-benzimidazole 
• 7711-39-9 benzimidazole-4,7-dione 
• 92800-19-6 4,7-dimethoxy-1(3)H-benzimidazol-5-ylamine 

Relevant academic research and scientific papers

Diastereospecific enolate addition and atom-efficient benzimidazole synthesis for the production of l/t calcium channel blocker act-280778

A scalable access to 1 (ACT-280778), a potent L/T calcium channel blocker, has been developed. The synthesis, amenable to kilogram manufacturing, comprises 10 chemical steps from enantiomerically pure 5-phenylbicyclo[2.2.2]oct-5-en-2-one (3) and 1,4-dimethoxybenzene with a longest linear sequence of 7 steps. Key to the success of this fit-for-purpose approach are a robust and atom-efficient access to benzimidazole 4, the substrate-controlled diastereoselective enolate addition toward carboxylic acid 2 that was isolated by simple crystallization with high dr (>99:1), the convenient selective N-deacylation of intermediate 10, and the identification of a suitable solid form of 1 as the bis-maleate salt (1·2 C4H4O4). As an illustration of the robustness of this process, 14 kg of drug substance, suitable for human use, was produced with an overall yield of 38% over the longest linear sequence (7 steps).

An improved methodology for the preparation of 4,7-dimethoxy-1H- benzimidazole, a key intermediate in the synthesis of 1-alkyl-1H-benzimidazole- 4,7-diones

We reported an optimized process for the preparation of key intermediate, 4,7-dimethoxy-1H-benzimidazole, from commercially available 1,4-dimethoxybenzene (Overall yield 52%). We successfully applied this methodology to an improved synthesis of 1-benzyl-1

Benzimidazole-4,7-diones as inhibitors of protozoal (Toxoplasma gondii) purine nucleoside phosphorylase

Benzimidazole-4,7-diones derivatives substituted at 1- and/or 2-position have been synthetized and tested as inhibitors of purine nucleoside phosphorylase (PNP), isolated from two strains of Toxoplasma gondii (RH and ME 49). They were identified as inhibi