26561-15-9

Upstream product

• 5888-52-8 4-propyl-1,2-dimethoxybenzene 
• 3535-37-3 3,4-dimethoxybenzoic acid chloride 
• 2785-87-7 2-methoxy-4-n-propylphenol 
• 121-34-6 3-methoxy-4-hydroxybenzoic acid 
• 77-78-1 dimethyl sulfate 
• 93-07-2 Veratric acid 

Downstream Products

• 26561-16-0 1-(3,4-Dimethoxy-phenyl)-1-(3,4-dimethoxy-6-propyl-phenyl)-1-propanol 
• 26561-17-1 1-(3,4-Dimethoxy-phenyl)-1-(3,4-dimethoxy-6-propyl-phenyl)-propan 
• 22345-47-7 tofisopam 
• 41565-05-3 4,5-dimethoxy-2-veratroyl-benzoic acid methyl ester 
• 102719-50-6 2-(3,4-dimethoxybenzoyl)-4,5-dimethoxypropiophenone 

Relevant academic research and scientific papers

Synthesis of Tofisopam by Way of Photoinduced CO2 Fixation

Herein reported is a unique synthetic route of Tofisopam, an anxiolytic drug containing a 2,3-benzodiazepine core structure. 3,4-Dimethoxypropylbenzene and 3,4-dimethoxybenzoic acid, which are both of plant origin, and CO2 constitute its carbon skeleton. These three renewable substances are united by two C?C bond forming reactions, i.e., a Friedel–Crafts acylation reaction and a photoinduced carboxylation reaction to construct the major carbon framework. Finally, a methyl group is introduced by a Kumada-type cross-coupling reaction to furnish Tofisopam. Various analogs of Tofisopam are readily synthesized by introducing other substituents than a methyl group at the last C?C bond forming step.

PRODUCTION METHOD OF TOFISOPAM, INTERMEDIATE THEREOF, AND PRODUCTION METHOD OF THE INTERMEDIATE

To provide: a method for performing optical carboxylation of o-alkyl benzophenone at a high reaction rate and high yield by a simpler operation; and a method for producing tofisopam at low cost.SOLUTION: There is produced 2,3-benzodiazepine derivative (to