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BCPPlus SIGNED

New directions in bicyclopentane research

Total Cost €

0

EC-Contrib. €

0

Partnership

0

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 BCPPlus project word cloud

Explore the words cloud of the BCPPlus project. It provides you a very rough idea of what is the project "BCPPlus" about.

invention    routes    susceptibility    tcp    derivatives    tactics    transfer    directionality    metabolic    chemistry    exhibit    substituent    previously    scaffolds    lack    diameters    candidates    bicyclo    receiving    revolutionize    aryl    generalized    radical    activation    positioning    explored    attractive    accessible    solution    organic    space    occupy    subject    natural    syntheses    ring    template    analogues    additionally    drug    property       bcps    inaccessible    modification    mimic    immature    pharmaceutical    biological    nature    industrial    structural    pentane    explore    motifs    rigid    medicinal    tricyclopentane    despite    bcp    functionalize    functionalization    themselves    edge    seeking    relative    pharmacological    cutting    industry    drugs    reaction    bioisosteres    atra    parent    strategy    dimensions    polysubstituted    date    area    alkyl    mild    intellectual    halides    contemporary       atom    opening    synthesize    found    arene    pharmacokinetic    hetero    abundance    polycycles    expanded   

Project "BCPPlus" data sheet

The following table provides information about the project.

Coordinator
THE CHANCELLOR, MASTERS AND SCHOLARS OF THE UNIVERSITY OF OXFORD 

Organization address
address: WELLINGTON SQUARE UNIVERSITY OFFICES
city: OXFORD
postcode: OX1 2JD
website: www.ox.ac.uk

contact info
title: n.a.
name: n.a.
surname: n.a.
function: n.a.
email: n.a.
telephone: n.a.
fax: n.a.

 Coordinator Country United Kingdom [UK]
 Total cost 183˙454 €
 EC max contribution 183˙454 € (100%)
 Programme 1. H2020-EU.1.3.2. (Nurturing excellence by means of cross-border and cross-sector mobility)
 Code Call H2020-MSCA-IF-2017
 Funding Scheme MSCA-IF-EF-ST
 Starting year 2018
 Duration (year-month-day) from 2018-07-02   to  2020-07-01

 Partnership

Take a look of project's partnership.

# participants  country  role  EC contrib. [€] 
1    THE CHANCELLOR, MASTERS AND SCHOLARS OF THE UNIVERSITY OF OXFORD UK (OXFORD) coordinator 183˙454.00

Map

 Project objective

The pharmaceutical industry is increasingly seeking new tactics for the structural modification of drug candidates to avoid metabolic susceptibility, or to improve pharmacokinetic properties. Analogues called 'bioisosteres', which mimic the dimensions and substituent directionality of problematic structural motifs, but which are not themselves subject to the same pharmacological issues, offer one solution. Often based on scaffolds not found in ‘typical’ drug candidates, bioisosteres can additionally occupy new areas of intellectual property space. Within this growing field, rigid polycycles such as bicyclo[1.1.1]pentane (BCP) are receiving significant attention as arene bioisosteres, as they exhibit similar ring diameters and substituent positioning, and also improve many pharmacokinetic properties relative to the parent arene. Despite the attractive nature of these motifs and current interest, the lack of general routes to complex BCP ring systems means this template is not yet fully accessible to industry. The invention of mild methods for [1.1.1.0]tricyclopentane (TCP) ring opening and functionalization could revolutionize use of BCPs in the pharmaceutical sector. One method not explored to date is an atom transfer radical addition reaction (ATRA) strategy. Using aryl or alkyl halides, ATRA could deliver an abundance of previously inaccessible polysubstituted BCPs from generalized TCP, which would revolutionize this immature, cutting-edge area of organic and medicinal chemistry. This research proposal seeks to: i) explore general and mild ATRA-based syntheses of BCP derivatives, including ring-expanded (hetero)bioisosteres; ii) functionalize BCP products using a range of contemporary processes, including C–H or C–X activation; and iii) apply these methodologies to synthesize BCP drugs / natural product analogues, and to test their biological activity via an industrial collaboration.

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The information about "BCPPLUS" are provided by the European Opendata Portal: CORDIS opendata.

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