Asymmetric synthesis of pyrrolidine-containing chemical scaffolds via Tsuji-Trost allylation of N-tert-butanesulfinyl imines

A simple and efficient asymmetric synthesis of novel sp3 rich pyrrolidine chemical scaffolds over five steps starting from simple ketones is described. Key steps involve the use of tert-butanesulfinamide as a chiral auxiliary to perform an asymmetric Tsuji-Trost allylation, with subsequent cross-met...

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Main Authors: Dawood, Rafid S., Georgiou, Irene, Wilkie, Ross P., Lewis, William, Stockman, Robert A.
Format: Article
Published: Wiley-VCH Verlag 2017
Online Access:https://eprints.nottingham.ac.uk/46526/
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author Dawood, Rafid S.
Georgiou, Irene
Wilkie, Ross P.
Lewis, William
Stockman, Robert A.
author_facet Dawood, Rafid S.
Georgiou, Irene
Wilkie, Ross P.
Lewis, William
Stockman, Robert A.
author_sort Dawood, Rafid S.
building Nottingham Research Data Repository
collection Online Access
description A simple and efficient asymmetric synthesis of novel sp3 rich pyrrolidine chemical scaffolds over five steps starting from simple ketones is described. Key steps involve the use of tert-butanesulfinamide as a chiral auxiliary to perform an asymmetric Tsuji-Trost allylation, with subsequent cross-metathesis with an acrylate ester and reduction of the sulfinimine/cyclisation of the resulting amine giving the pyrrolidine scaffolds in high yields and diastereoselectivites. By removing the chiral auxiliary and functionalising the ester group, the resulting scaffold core can be further derivatised.
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institution University of Nottingham Malaysia Campus
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publishDate 2017
publisher Wiley-VCH Verlag
recordtype eprints
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spelling nottingham-465262020-05-04T19:00:41Z https://eprints.nottingham.ac.uk/46526/ Asymmetric synthesis of pyrrolidine-containing chemical scaffolds via Tsuji-Trost allylation of N-tert-butanesulfinyl imines Dawood, Rafid S. Georgiou, Irene Wilkie, Ross P. Lewis, William Stockman, Robert A. A simple and efficient asymmetric synthesis of novel sp3 rich pyrrolidine chemical scaffolds over five steps starting from simple ketones is described. Key steps involve the use of tert-butanesulfinamide as a chiral auxiliary to perform an asymmetric Tsuji-Trost allylation, with subsequent cross-metathesis with an acrylate ester and reduction of the sulfinimine/cyclisation of the resulting amine giving the pyrrolidine scaffolds in high yields and diastereoselectivites. By removing the chiral auxiliary and functionalising the ester group, the resulting scaffold core can be further derivatised. Wiley-VCH Verlag 2017-08-16 Article PeerReviewed Dawood, Rafid S., Georgiou, Irene, Wilkie, Ross P., Lewis, William and Stockman, Robert A. (2017) Asymmetric synthesis of pyrrolidine-containing chemical scaffolds via Tsuji-Trost allylation of N-tert-butanesulfinyl imines. Chemistry - a European Journal, 23 (46). pp. 11153-11158. ISSN 1521-3765 http://onlinelibrary.wiley.com/doi/10.1002/chem.201702616/abstract doi:10.1002/chem.201702616 doi:10.1002/chem.201702616
spellingShingle Dawood, Rafid S.
Georgiou, Irene
Wilkie, Ross P.
Lewis, William
Stockman, Robert A.
Asymmetric synthesis of pyrrolidine-containing chemical scaffolds via Tsuji-Trost allylation of N-tert-butanesulfinyl imines
title Asymmetric synthesis of pyrrolidine-containing chemical scaffolds via Tsuji-Trost allylation of N-tert-butanesulfinyl imines
title_full Asymmetric synthesis of pyrrolidine-containing chemical scaffolds via Tsuji-Trost allylation of N-tert-butanesulfinyl imines
title_fullStr Asymmetric synthesis of pyrrolidine-containing chemical scaffolds via Tsuji-Trost allylation of N-tert-butanesulfinyl imines
title_full_unstemmed Asymmetric synthesis of pyrrolidine-containing chemical scaffolds via Tsuji-Trost allylation of N-tert-butanesulfinyl imines
title_short Asymmetric synthesis of pyrrolidine-containing chemical scaffolds via Tsuji-Trost allylation of N-tert-butanesulfinyl imines
title_sort asymmetric synthesis of pyrrolidine-containing chemical scaffolds via tsuji-trost allylation of n-tert-butanesulfinyl imines
url https://eprints.nottingham.ac.uk/46526/
https://eprints.nottingham.ac.uk/46526/
https://eprints.nottingham.ac.uk/46526/