Skeletal editing approach to bridge-functionalized Bicyclo [1.1. 1] pentanes from Azabicyclo [2.1. 1] hexanes

…, MK Ameriks, R Sarpong, TP Lebold - Journal of the …, 2023 - ACS Publications
Azabicyclo[2.1.1]hexanes (aza-BCHs) and bicyclo[1.1.1]pentanes (BCPs) have emerged as
attractive classes of sp 3 -rich cores for replacing flat, aromatic groups with metabolically …

Intramolecular annulations of donor–acceptor cyclopropanes

TP Lebold, MA Kerr - Pure and Applied Chemistry, 2010 - degruyter.com
… TP LEBOLD AND MA KERR … TP LEBOLD AND MA KERR … Removal of the p-methoxybenzyl
(PMB) group with dichlorodicyano-p-benzoquinone (DDQ), followed by mesylation of the …

Zn (II)-catalyzed synthesis of piperidines from propargyl amines and cyclopropanes

TP Lebold, AB Leduc, MA Kerr - Organic letters, 2009 - ACS Publications
The reaction of benzyl-protected propargyl amines and 1,1-cyclopropane diesters in the
presence of catalytic Zn(NTf 2 ) 2 allows access to highly functionalized piperidines in excellent …

Tandem Cyclopropane ring-opening/Conia-ene reactions of 2-alkynyl indoles: A [3+ 3] annulative route to tetrahydrocarbazoles

HK Grover, TP Lebold, MA Kerr - Organic Letters, 2011 - ACS Publications
A Zn(NTf 2 ) 2 catalyzed tandem reaction consisting of a nucelophilic ring opening of 1,1-cyclopropanediesters
by 2-alkynyl indoles followed by a Conia-ene ring closure results in the …

A selective orexin-1 receptor antagonist attenuates stress-induced hyperarousal without hypnotic effects

…, A Shekhar, SD Fitz, BT Shireman, TP Lebold… - … of Pharmacology and …, 2015 - ASPET
Orexins (OXs) are peptides produced by perifornical (PeF) and lateral hypothalamic neurons
that exert a prominent role in arousal-related processes, including stress. A critical role for …

Selective orexin receptor antagonists

TP Lebold, P Bonaventure, BT Shireman - Bioorganic & medicinal …, 2013 - Elsevier
The orexin, or hypocretin, neuropeptides (orexin-A and orexin-B) are produced on neurons
in the hypothalamus which project to key areas of the brain that control sleep–wake states, …

A Unifying Synthesis Approach to the C18-, C19-, and C20-Diterpenoid Alkaloids

…, BX Li, GM Gallego, TP Lebold… - Journal of the …, 2017 - ACS Publications
The secondary metabolites that comprise the diterpenoid alkaloids are categorized into C
18 , C 19 , and C 20 families depending on the number of contiguous carbon atoms that …

A benzyne insertion approach to hetisine-type diterpenoid alkaloids: synthesis of cossonidine (davisine)

…, LC Morrill, EL Fisher, K Clagg, TP Lebold… - Journal of the …, 2018 - ACS Publications
The hetisine-type natural products exhibit one of the most complex carbon skeletons within
the diterpenoid alkaloid family. The use of network analysis has enabled a synthesis strategy …

[HTML][HTML] Translational evaluation of novel selective orexin-1 receptor antagonist JNJ-61393215 in an experimental model for panic in rodents and humans

…, PL Johnson, B Lord, BT Shireman, TP Lebold… - Translational …, 2020 - nature.com
Orexin neurons originating in the perifornical and lateral hypothalamic area project to
anxiety- and panic-associated neural circuitry, and are highly reactive to anxiogenic stimuli. …

A divergent approach to the synthesis of the yohimbinoid alkaloids venenatine and alstovenine

TP Lebold, JL Wood, J Deitch, MW Lodewyk… - Nature …, 2013 - nature.com
The yohimbinoid alkaloids continue to receive considerable attention from the synthetic
community because of their interesting chemical structures and varied biological activity. …