Cuprate addition to a 6-substituted pentafulvene: preparation of sec-alkyl substituted titanocene dichlorides and their biological activity

The copper-catalysed (10 mol-% CuBr·SMe2, CuCN·LiCl or CuI/PPh3) addition of RMgBr to the pentafulvene 1-(cyclopenta-2,4-dien-1-ylidenemethyl)-2-methoxybenzene allows the formation of cyclopentadienyl derivatives with α-CHR(2-MeOPh) sidechains (R = Me, Et, nBu, iBu, allyl, Ph) without H– transfer. T...

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Main Authors: Cini, Melchior, Bradshaw, Tracey D., Lewis, William, Woodward, Simon
Format: Article
Published: Wiley-VCH Verlag 2013
Online Access:https://eprints.nottingham.ac.uk/3200/
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author Cini, Melchior
Bradshaw, Tracey D.
Lewis, William
Woodward, Simon
author_facet Cini, Melchior
Bradshaw, Tracey D.
Lewis, William
Woodward, Simon
author_sort Cini, Melchior
building Nottingham Research Data Repository
collection Online Access
description The copper-catalysed (10 mol-% CuBr·SMe2, CuCN·LiCl or CuI/PPh3) addition of RMgBr to the pentafulvene 1-(cyclopenta-2,4-dien-1-ylidenemethyl)-2-methoxybenzene allows the formation of cyclopentadienyl derivatives with α-CHR(2-MeOPh) sidechains (R = Me, Et, nBu, iBu, allyl, Ph) without H– transfer. The deprotonation of these sec-alkyl-substituted cyclopentadienyls followed by the addition of TiCl4 allows the isolation of TiCl2{η5-C5H4CHR(2-OMePh)} as rac/meso mixtures that show activity against human colon, breast and pancreatic cell lines (GI50 2.3–42.4 μM).
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spelling nottingham-32002020-05-04T16:37:14Z https://eprints.nottingham.ac.uk/3200/ Cuprate addition to a 6-substituted pentafulvene: preparation of sec-alkyl substituted titanocene dichlorides and their biological activity Cini, Melchior Bradshaw, Tracey D. Lewis, William Woodward, Simon The copper-catalysed (10 mol-% CuBr·SMe2, CuCN·LiCl or CuI/PPh3) addition of RMgBr to the pentafulvene 1-(cyclopenta-2,4-dien-1-ylidenemethyl)-2-methoxybenzene allows the formation of cyclopentadienyl derivatives with α-CHR(2-MeOPh) sidechains (R = Me, Et, nBu, iBu, allyl, Ph) without H– transfer. The deprotonation of these sec-alkyl-substituted cyclopentadienyls followed by the addition of TiCl4 allows the isolation of TiCl2{η5-C5H4CHR(2-OMePh)} as rac/meso mixtures that show activity against human colon, breast and pancreatic cell lines (GI50 2.3–42.4 μM). Wiley-VCH Verlag 2013-06-19 Article PeerReviewed Cini, Melchior, Bradshaw, Tracey D., Lewis, William and Woodward, Simon (2013) Cuprate addition to a 6-substituted pentafulvene: preparation of sec-alkyl substituted titanocene dichlorides and their biological activity. European Journal of Organic Chemistry, 2013 (19). pp. 3997-4007. ISSN 1099-0690 http://onlinelibrary.wiley.com/doi/10.1002/ejoc.201300474/abstract
spellingShingle Cini, Melchior
Bradshaw, Tracey D.
Lewis, William
Woodward, Simon
Cuprate addition to a 6-substituted pentafulvene: preparation of sec-alkyl substituted titanocene dichlorides and their biological activity
title Cuprate addition to a 6-substituted pentafulvene: preparation of sec-alkyl substituted titanocene dichlorides and their biological activity
title_full Cuprate addition to a 6-substituted pentafulvene: preparation of sec-alkyl substituted titanocene dichlorides and their biological activity
title_fullStr Cuprate addition to a 6-substituted pentafulvene: preparation of sec-alkyl substituted titanocene dichlorides and their biological activity
title_full_unstemmed Cuprate addition to a 6-substituted pentafulvene: preparation of sec-alkyl substituted titanocene dichlorides and their biological activity
title_short Cuprate addition to a 6-substituted pentafulvene: preparation of sec-alkyl substituted titanocene dichlorides and their biological activity
title_sort cuprate addition to a 6-substituted pentafulvene: preparation of sec-alkyl substituted titanocene dichlorides and their biological activity
url https://eprints.nottingham.ac.uk/3200/
https://eprints.nottingham.ac.uk/3200/