KETENCYCLS

Biomimetic Late Stage Aromatisation Reactions: from Cancer Chemotherapy to Novel Polymers

Coordinatore	more Spiacenti, non ci sono informazioni su questo coordinatore. Contattare Fabio per maggiori infomrazioni, grazie.
Nazionalità Coordinatore	Non specificata
Totale costo	1˙960˙938 €
EC contributo	1˙960˙938 €
Programma	FP7-IDEAS-ERC Specific programme: "Ideas" implementing the Seventh Framework Programme of the European Community for research, technological development and demonstration activities (2007 to 2013)
Code Call	ERC-2010-AdG_20100224
Funding Scheme	ERC
Anno di inizio	2011
Periodo (anno-mese-giorno)	2011-03-01   -   2016-02-29

 Partecipanti

#	participant	country	role	EC contrib. [€]
1	IMPERIAL COLLEGE OF SCIENCE, TECHNOLOGY AND MEDICINE  Organization address address: SOUTH KENSINGTON CAMPUS EXHIBITION ROAD city: LONDON postcode: SW7 2AZ contact info Titolo: Ms. Nome: Brooke Cognome: Alasya Email: send email Telefono: +44 207 594 1181 Fax: +44 207 594 1418	UK (LONDON)	hostInstitution	1˙960˙938.00
2	IMPERIAL COLLEGE OF SCIENCE, TECHNOLOGY AND MEDICINE  Organization address address: SOUTH KENSINGTON CAMPUS EXHIBITION ROAD city: LONDON postcode: SW7 2AZ contact info Titolo: Prof. Nome: Anthony Gerard Martin Cognome: Barrett Email: send email Telefono: +44 207 594 5767 Fax: +44 207 594 5805	UK (LONDON)	hostInstitution	1˙960˙938.00

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 Obiettivo del progetto (Objective)

'The applicant is seeking funding to support research on late stage biomimetic syntheses of resorcylates from readily available non-aromatic precursors. A series of diketo-dioxinones will be synthesised using mild Claisen condensation reactions and converted into the reactive intermediates triacyl-ketenes by retro-Diels Alder reactions. These will be trapped with alcohols to directly provide the corresponding resorcylate esters and related macrocyclic lactones. These compounds are of considerable importance in that they occur in structurally complex natural products, which are active as anticancer agents, antibiotics, immunosuppressants or analgesics. Examples include aigialomycin D, radicicol, cruentaren A and mycophenolic acid. Late aromatisation avoids the severe problems associated with existing syntheses based on aromatic precursors. Our studies will allow for the development of very concise total syntheses of the biologically potent Hsp90 inhibitor radicicol and mitochondrial F-ATPase inhibitor cruentaren A. The methods will be amenable for the synthesis of libraries of synthetic natural product analogues in the quest for superior drugs to treat cancer. The novel ring opening, ring closing and crossed metathesis of cyclooctyne derivatives will be introduced and will simplify the route to cruentaren A. Resorcylate methodology will be extended to terpenoid-resorcylates, using a new decarboxylative allyl transfer process, which will greatly simplify routes to angelicoin A, cristatic acid, mycophenolic acid and hongoquercin B. Finally, both the aromatisation strategy and ring opening metathesis polymerisation of cyclooctyne derivatives will be applied in the synthesis of novel oligomers and polymers including polyfunctional polyesters and poly-ynes.'