Investigation of Various Organocatalysts for Improved and Efficient One Pot Synthesis of 2,3-Dihydro-1H-1,5-benzodiazepines Under Solvent-Free Condition

Yuhao Zhao1,†, Shikha Sharma2,†, Minghua Huang3, Akshdeep Sandhar2, Rajesh K. Singh2,* and Yanxu Ma3,*

1School of Traditional Chinese Medicine, Capital Medical University, Beijing 100069, P.R. China

2Department of Pharmaceutical Chemistry, Shivalik College of Pharmacy (Under Local Govt. Dept. Punjab) Nangal, Distt. Rupnagar-140126, Punjab, India

3Department of Orthopedics, Beijing Traditional Chinese Medicine Hospital, Capital Medical University, Beijing 100010, P.R. China

*Corresponding authors: E-mail: rksingh244@gmail.com; yizhangchaimen@gmail.com

†Authors contributed equally this work

Abstract

A series of 2,3-dihydro-1H-1,5-benzodiazepines derivatives were synthesized by one-pot three-components condensation reaction of o-phenylenediamines with a,b-unsaturated carbonyl compounds and effect of various Brønsted organo acids as catalyst was studied. Among the various organo acids screened, trifluoroacetic acid is versatile catalyst and the corresponding products were obtained in good to excellent yield (84-94 %) under solvent-free condition.

Keywords

1,5-Benzodiazepines, Organoacids, Trifluoroacetic acid, One pot, Solvent-free, Green chemistry.

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