An expeditious protocol for synthesis of Baylis–Hillman derived piperazine derivatives and evaluation of their AChE inhibition

The highly efficient and eco-economical “on water” method has been developed for the rapid construction of highly functionalized Baylis–Hillman derived piperazine derivatives ( n  = 34) in excellent yields under mild, catalyst-free reaction conditions. All the synthesized compounds were further scre...

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Bibliographic Details
Published in:Research on chemical intermediates 2018, Vol.44 (1), p.553-565
Main Authors: Bikshapathi, Raktani, Sai Prathima, Parvathaneni, Yashwanth, Bomma, Rajesh, Pamanji, Rao, Janapala Venkateswara, Jagadeesh Kumar, Gangasani, Jagadeesh, Nanubolu, Rao, Vaidya Jayathirtha
Format: Article
Language:English
Subjects:
Catalysis
Chemical synthesis
Chemistry
Chemistry and Materials Science
Crystal structure
Derivatives
Inorganic Chemistry
Physical Chemistry
Substrates
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Summary:The highly efficient and eco-economical “on water” method has been developed for the rapid construction of highly functionalized Baylis–Hillman derived piperazine derivatives ( n  = 34) in excellent yields under mild, catalyst-free reaction conditions. All the synthesized compounds were further screened for in vitro ACE inhibitor activity. This process has a broad substrate scope, is operationally simple, generally requires no chromatographic purification, is scalable and is significantly greener than current alternatives. The molecular and crystal structures of new piperazine derivative 3r have been investigated. The synthesised compounds exhibit several structural features that make them promising candidates as biologically active compounds.
ISSN:0922-6168
1568-5675
DOI:10.1007/s11164-017-3119-9