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Title:
MICROWAVE INDUCED SINGLE STEP GREEN SYNTHESIS OF SOME NOVEL 2-ARYL ALDEHYDES AND THEIR ANALOGUES
Document Type and Number:
WIPO Patent Application WO/2010/097811
Kind Code:
A4
Abstract:
The present invention provides a process for the preparation of some novel 2-aryl and 2,2-diaryl aldehydes and analogues which are privileged intermediates for commercially important nonsteroidal anti-inflammatory drugs including naproxen, flurbiprofen and potent anticancer drug candidates, including phenstatin through a unique single step synthetic methodology utilizing easily available substrates in the form of aryl alkenes as well as environmentally benign aqueous reaction conditions in the form of solvents such as mixtures of water and DMSO or Dioxane and reagents N-bromosuccinimide, N- iodosuccinimide, N-cholorosuccinimide and phase transfer catalyst such as cetyltrimethyl ammonium bromide, N-hexyl ammonium chloride for a reaction time varying from 1min- 30min, depending upon microwave or conventional heating, without using expensive transition metal catalysts or lewis acids/bases with yield varying from 35-55 %, depending upon the solvent and substrate used. The developed method provides a clean and convenient alternative to access a diverse range of medicinally important 2-aryl and 2,2- diaryl aldehyde based scaffolds in lieu of the conventional multistep protocols employing expensive and hazardous transition metal catalysts and lewis acids/bases.

Inventors:
SINHA, Arun, Kumar (Institute of Himalayan Bioresource Technology, P.O.Box No.6Palampur 1, Himachal Pradesh, 170 06, IN)
SHARMA, Abhishek (Institute of Himalayan Bioresource Technology, P.O.Box No.6Palampur 1, Himachal Pradesh, 170 06, IN)
KUMAR, Rakesh (Institute of Himalayan Bioresource Technology, P.O.Box No.6Palampur 1, Himachal Pradesh, 170 06, IN)
SHARMA, Naina (Institute of Himalayan Bioresource Technology, P.O.Box No.6Palampur 1, Himachal Pradesh, 170 06, IN)
Application Number:
IN2010/000110
Publication Date:
November 04, 2010
Filing Date:
February 25, 2010
Export Citation:
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Assignee:
COUNCIL OF SCIENTIFIC & INDUSTRIAL RESEARCH (Anusandhan Bhawan, 2 Rafi Marg, New Delhi 1, 110 00, IN)
SINHA, Arun, Kumar (Institute of Himalayan Bioresource Technology, P.O.Box No.6Palampur 1, Himachal Pradesh, 170 06, IN)
SHARMA, Abhishek (Institute of Himalayan Bioresource Technology, P.O.Box No.6Palampur 1, Himachal Pradesh, 170 06, IN)
KUMAR, Rakesh (Institute of Himalayan Bioresource Technology, P.O.Box No.6Palampur 1, Himachal Pradesh, 170 06, IN)
SHARMA, Naina (Institute of Himalayan Bioresource Technology, P.O.Box No.6Palampur 1, Himachal Pradesh, 170 06, IN)
International Classes:
C07C45/30; C07C47/228; C07C47/23; C07C47/24; C07C47/277; C07C311/49; C07D317/54
Attorney, Agent or Firm:
LALL, Amar, Raj (LALL LAHIRI & SALHOTRA, Plot No. B-28 Sector-32,Institutional Area,Gurgaon 1, Haryana, 122 00, IN)
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