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TitleOne pot process for the arylation of beta-dicarbonyl compounds to produce a diverse range of complex bioactive natural products
Knowhow is available forA transition-metal-free, chemo-selective, one pot process for the C- arylation of malonamide esters at room temperature with good yield
SummaryThe alpha-arylation of active methylene carbonyl compounds has become a widely used method, which provides an easy access to important classes of biologically active natural/synthetic products.
CSIR-NCL scientists have developed a one pot, room temperature process for the C-arylation of beta-dicarbonyl ester-amide compounds in presence of CsF and anhydrous polar organic solvent, optionally in presence of additives to obtain desired arylated dicarbonyl compounds with good yield.
It is observed that the standardized arylation protocol could be applied for the generation of quaternary stereocenters, which are found in several important and useful molecules in pharmaceutical and medicinal applications, as well as in many natural products. Construction of such quaternary stereocenters is much more demanding and challenging task. The malonamide ester containing p-chloroaniline provides high yields at milder reaction condition.
Advantages- The instant chemo-selective process is performed at room temperature and in one pot
- The reaction to take place at room temperature in few hours, in mild conditions
- Reaction used simple, further easily available reagents are employed and expensive transition metal catalyst is avoided
- The instant arylation process is cost effective and industrially viable to obtain high yield of arylated dicarbonyl compounds

Knowhow is listed under following categories

Knowhow from
Scientific/ engineering subject areas Chemical sciences & engineering
Investor interest categories Biotechnology/ Biomedical/ Health Technologies
Industries Organic Chemicals, Fine Chemicals, Intermediates, Feedstocks
Customer categories and nature of business Businesses and other industries (B2B)
Technology readiness levels TRL C: Prototype developed and tested; technology demonstrated at pilot scale

Year of development
Whether patents are part of this offering ?Yes

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Published Patents

Database reference

Database record number 20140423022840
Date of upload 23 / Apr / 2014
Date of update 2 / May / 2014
URL to site when communicating about this knowhow http://nclinnovations.org/khdb/viewrecord.php?recordno=20140423022840
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