The Experts below are selected from a list of 288 Experts worldwide ranked by ideXlab platform
Philip Thorne - One of the best experts on this subject based on the ideXlab platform.
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concise synthesis of novel 2 6 diazaspiro 3 3 heptan 1 ones and their conversion into 2 6 diazaspiro 3 3 Heptanes
Synlett, 2007Co-Authors: Michael J Stocks, Daniel Hamza, Garry Pairaudeau, Jeffrey P Stonehouse, Philip ThorneAbstract:A concise synthesis, amenable to library production of 2,6-diazaspiro[3.3]heptan-1-ones and their subsequent conversion into 2,6-diazaspiro[3.3]Heptanes is reported.
P Viani - One of the best experts on this subject based on the ideXlab platform.
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novel n aryl nicotinamide derivatives taking stock on 3 6 diazabicyclo 3 1 1 Heptanes as ligands for neuronal acetylcholine receptors
European Journal of Medicinal Chemistry, 2019Co-Authors: Gabriele Murineddu, Cecilia Gotti, Battistina Asproni, Paola Corona, Katiuscia Martinello, Simona Plutino, Sergio Fucile, Veronika Temml, Milena Moretti, P VianiAbstract:Abstract We designed the synthesis of a small library of 3-substituted-3,6-diazabicyclo[3.1.1]Heptanes whose affinity on neuronal nicotinic receptors (nAChRs) was evaluated. Among the synthesized compounds, the 5-(3,6-diazabicyclo[3.1.1]heptane-3-yl)- N -(2-fluorophenyl)nicotinamide 43 proved to be the most interesting compound with α 4 β 2 Ki value of 10 pM and a very high α 7 /α 4 β 2 selectivity. Furthermore, compounds 35 , 39 and 43 elicited a selective partial agonist activity for α 4 β 2 nAChR subtype. Finally, in this paper we also report the conclusions on the 3,6-diazabicyclo[3.1.1]Heptanes as ligands for nAChRs, resulting from our consolidated structure activity relationship (SAR) studies on this template.
Erick M Carreira - One of the best experts on this subject based on the ideXlab platform.
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2 6 diazaspiro 3 3 Heptanes synthesis and application in pd catalyzed aryl amination reactions
Organic Letters, 2008Co-Authors: Johannes A Burkhard, Erick M CarreiraAbstract:A concise and scalable synthesis of a 2,6-diazaspiro[3.3]heptane building block is reported. The usefulness of this structural surrogate of piperazine is shown in arene amination reactions yielding a variety of N-Boc-N′-aryl-2,6-diazaspiro[3.3]Heptanes.
Matthew W Bedore - One of the best experts on this subject based on the ideXlab platform.
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concise synthesis of n3 and n6 monoprotected 3 6 diazabicyclo 3 1 1 Heptanes useful intermediates for the preparation of novel bridged bicyclic piperazines
Tetrahedron Letters, 2012Co-Authors: Daniel P Walker, Matthew W BedoreAbstract:Abstract Bridged bicyclic piperazines are important building blocks in medicinal chemistry research. The bicyclic piperazine 3,6-diazabicylo[3.1.1]heptane is of particular interest as a piperazine isostere because it is achiral and shows similar lipophilicity to that of piperazine based on the c Log P of a derived analog. A concise synthesis of N 3 - and N 6 -monoprotected 3,6-diazabicyclo[3.1.1]Heptanes 2d and 2e , respectively, is described. The seven step sequence begins with inexpensive starting materials and uses straightforward chemistry.
Michael J Stocks - One of the best experts on this subject based on the ideXlab platform.
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concise synthesis of novel 2 6 diazaspiro 3 3 heptan 1 ones and their conversion into 2 6 diazaspiro 3 3 Heptanes
Synlett, 2007Co-Authors: Michael J Stocks, Daniel Hamza, Garry Pairaudeau, Jeffrey P Stonehouse, Philip ThorneAbstract:A concise synthesis, amenable to library production of 2,6-diazaspiro[3.3]heptan-1-ones and their subsequent conversion into 2,6-diazaspiro[3.3]Heptanes is reported.
