Synthesis and antitussive activity of obtucarbamate A derivatives

Abstract

Obtucarbamate A was purified from Disporum cantoniense with good antitussive property. In present work, a series of obtucarbamate A derivatives were designed and synthesized from obtucarbamate A by microwave method, and their antitussive activity were evaluated. The results showed that the toluene diisocyanate was obtained with a yield of 95.1% using a simple method, 1-methyl-2-pyrrolidinone as solvent, temperature of 190 °C, microwave irradiation at 60 W power for 30 min. All compounds have good antitussive activity, and small steric hindrance unsaturated groups of ester chains and amino groups favor activity. It is the first reported of obtucarbamate A derivatives used as antitussive, and the results provide a basis for the application of obtucarbamate derivatives as new antitussive.

Graphical Abstract

Keywords:

• Antitussive action
• microwave reaction
• obtucarbamate A
• structural modification
• toluene diisocyanate

Additional information

Funding

This work was supported by the Chunhui project of Ministry of Education [Grant No. (2013)2213] and the Construction Project of Key Laboratories from the Education Department of Guizhou Province [Grant No. QJHKY(2018)001].