A series of heterosubstitued alkynes was successfully submitted to the intramolecular carbolithiation of their triple bond. We show that the addition is stereoselective because of the control exerted by the terminal substituent X on the geometry of the transition state. A complementary DFT study suggests that the addition is anti when a strong Li-X interaction occurs.
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Chem Pharm Bull (Tokyo)
December 2024
Faculty of Pharmaceutical Sciences, Doshisha Women's College of Liberal Arts.
A total synthesis of javaberine A was achieved through a lithium amide-mediated intramolecular hydroamination of an N-allyl aminoalkene. The desired hydroamination was accomplished using an excess of i-PrNH with a substoichiometric amount of n-BuLi. Using an excess of both n-BuLi and i-PrNH led to tandem cyclization, however, resulting in the construction of a tricyclic structure through the formation of one C-N and two C-C bonds in a single operation.
View Article and Find Full Text PDFMolecules
June 2022
Department of Organic Chemistry, Faculty of Chemistry, University of Lodz, Tamka 12, 91-403 Lodz, Poland.
In this paper, we describe the lithiation of -benzylpyrene-1-carboxamide with RLi-TMEDA. We found that the reaction outcome strongly depends on the electrophile used in the quenching step. The electrophile can be introduced at either the benzylic position or at the C-2 position in the pyrene nucleus.
View Article and Find Full Text PDFJ Org Chem
July 2020
Institut des Molécules et Matériaux du Mans (IMMM)-UMR 6283 CNRS-Le Mans Université, Avenue Olivier Messiaen, Le Mans 72085, France.
-1,2-Cyclohexanediamine, -diether, and -amino ether were compared as chiral inducers in the asymmetric intramolecular carbolithiation of olefinic aryllithiums. Switching from diamine to ethereal ligands inverts the sense of asymmetric induction. This reversal of stereoselectivity was investigated through density functional theory calculations.
View Article and Find Full Text PDFOrg Lett
June 2018
Department of Chemistry , Ludwig-Maximilians-Universität, Butenandtstrasse 5-13 , 81377 Munich , Germany.
Various secondary alkyl iodides bearing a remote alkynylsilane underwent intramolecular carbolithiations triggered by an I/Li-exchange performed at -100 °C using t-BuLi (2.5 equiv). The resulting alkenyllithiums were stereoselectively converted to tetrasubstituted cyclopentane exo-alkylidenes.
View Article and Find Full Text PDFJ Org Chem
May 2017
Université du Maine and CNRS UMR 6283, Institut des Molécules et Matériaux du Mans , Faculté des Sciences et Techniques, avenue Olivier Messiaen, 72085 Le Mans Cedex 9, France.
A new class of chiral 1,2-amino ether ligands, readily accessible from naturally occurring α-amino- or α-hydroxy acids, was found to provide high levels of both conversion and stereocontrol (up to 95:5 er) in intramolecular carbolithiation reactions, outperforming the benchmark ligand (-)-sparteine. The ligand could be used in a substoichiometric amount (0.25 equiv) without significant loss of enantioselectivity.
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