A new approach to enantiopure β-endo-substituted azabicyclic proline analogues by base induced epimerization of a formyl derivative [PDF]
13 pages, 6 schemes, 1 figure.The β-epimer of methyl (1S,2R,4R)-N-benzoyl-2-formyl-7-azabicyclo[2.2.1]heptane-1- carboxylate, (1S, 2S, 4R)-7, has been obtained by treatment of the exo-formyl derivative with triethylamine in methanol. The development of
Buñuel, Elena +2 more
core +1 more source
This review summarizes recent advances in copper‐ and silver‐catalyzed reactions of active methylene isocyanides for the synthesis of highly substituted five‐ and six‐membered heterocycles. Emphasis is placed on [3+n] cycloadditions, annulations, and asymmetric strategies, highlighting current limitations and future opportunities in heterocycle ...
Jimil George, Kyungsoo Oh
wiley +1 more source
Discovery of Novel Adenosine Receptor Agonists That Exhibit Subtype Selectivity. [PDF]
A series of N(6)-bicyclic and N(6)-(2-hydroxy)cyclopentyl derivatives of adenosine were synthesized as novel A1R agonists and their A1R/A2R selectivity assessed using a simple yeast screening platform.
Dowell, Simon J +8 more
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2,3‐Dichloro‐5,6‐dicyano‐1,4‐benzoquinone serves as a versatile oxidant and redox catalyst for CC bond formation through hydride abstraction or single‐electron transfer. Stoichiometric and catalytic systems enable benzylic, allylic, and aromatic CH activation under mild, metal‐free conditions, providing sustainable routes to complex and bioactive ...
Dohoon Cha, Sun‐Joon Min
wiley +1 more source
Highly diastereoselective synthesis of 2-azabicyclo[2.2.1]hept-5-ene derivatives : bronsted acid catalized aza-diels-alder reaction between cyclopentadiene and imino-acetates with two chiral auxiliaries [PDF]
The cycloaddition between protonated glyoxylate imines possessing two chiral auxiliaries, N-(S)- or N-(R)-1-phenylethyl and (-)-8-phenylmenthyl or (+)-8- phenylneomenthyl, and cyclopentadiene is described.
Alves, M. José +3 more
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The new 2‐benzoylpyridine 4‐(bicyclo[2.2.1]hept‐2‐yl)thiosemicarbazone (HL) and its copper(II), nickel(II), cobalt(III), and iron(III) coordination compounds [Cu(L)Cl] (1), [Cu(L)NO3] (2), {[Cu(L)(Cl2CHCOO)]}n (3), [Ni(HL)2](NO3)2 (4), [Fe(L)2]NO3 (5), [Co(L)2]NO3 (6) were obtained.
Ianina Graur +6 more
wiley +1 more source
Structural differences determine the relative selectivity of nicotinic compounds for native α4β2^*-, α6β2^*-, α3β4^*- and α7-nicotine acetylcholine receptors [PDF]
Mammalian brain expresses multiple nicotinic acetylcholine receptor (nAChR) subtypes that differ in subunit composition, sites of expression and pharmacological and functional properties.
Bencherif, Merouane +10 more
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Anti-tumor and anti-angiogenic activity of novel hydantoin derivatives: Inhibition of VEGF secretion in liver metastatic osteosarcoma cells [PDF]
A series of new azaspiro bicyclic hydantoin derivatives has been designed and synthesized. Initially, the anti-proliferative effect of the hydantoin derivatives was evaluated against human ovarian cancer cells (SKOV-3 and OVSAHO) and murine osteosarcoma ...
Ananda Kumar, C.S. +4 more
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Synthesis and Activity of Six-Membered Cyclic Alkyl Amino Carbene–Ruthenium Olefin Metathesis Catalysts [PDF]
Ru–cyclic alkyl amino carbene (Ru–CAAC) olefin metathesis catalysts perform extraordinarily in metathesis macrocyclization and ethenolysis, but previous studies have been limited to the use of five-membered CAAC (CAAC-5) ligands.
Grubbs, Robert H. +4 more
core
An update on the synthesis and reactivity of spiro-fused β-lactams [PDF]
Beta-Lactam ring-containing compounds play a pivotal role in drug design and synthetic chemistry. Spirocyclic beta-lactams, representing an important beta-lactam subclass, have recently attracted considerable interest with respect to new synthetic ...
D'hooghe, Matthias, Dao Thi, Hang
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