Diversity-oriented synthesis of 1,3-benzodiazepines [PDF]
© 2017 Elsevier Ltd A concise assembly of the 1,3-benzodiazepine core from A 3 -coupling-derived propargylamines and ortho-bromophenylisocyanates is described.
Li, Binbin+7 more
core +2 more sources
Pharmaceutically relevant (hetero)cyclic compounds and natural products from lignin-derived monomers:Present and perspectives [PDF]
Lignin, the richest source of renewable aromatics on the planet, is an intriguing raw material for the construction of value-added aromatics. In the past decade, much progress has been made regarding the development of efficient lignin depolymerization ...
Afanasenko, Anastasiia, Barta, Katalin
core +1 more source
SPION nanoparticles for delivery of dopaminergic isoquinoline and benzazepine derivatives
Superparamagnetic iron nanoparticles (SPIONs) have become one of the most useful colloidal systems in nanomedicine. We report here the preparation of new hybrid core@shell systems based on SPION nanoparticles coated with a SiO2 shell (SPION@SiO2) and functionalized with carboxyl groups (SPION@SiO2-COOH).
Lucena-Serrano, Cristina+9 more
openaire +5 more sources
Fe‐Catalyzed α‐C(sp3)−H Amination of N‐Heterocycles
An iron(II)‐catalyzed α‐selective C−H amination of N‐heterocycles is reported. It employs the N‐heterocycle as the limiting reagent and presumably involves the formation of a reactive Fe‐nitrene/imidyl radical species. This operationally simple method is amenable to the late‐stage functionalization of natural products and APIs.
Andrea Geraci, Olivier Baudoin
wiley +2 more sources
Graph-Sparse LDA: A Topic Model with Structured Sparsity [PDF]
Originally designed to model text, topic modeling has become a powerful tool for uncovering latent structure in domains including medicine, finance, and vision.
Adams, Ryan+2 more
core +1 more source
Impact of spermiogram and sperm function test in idiopathic recurrent pregnancy loss [PDF]
Aims: To evaluate the role of sperm factors in idiopathic recurrent pregnancy loss cases. Methods: We recruited 100 male subjects where their female partners experienced 2 or more idiopathic pregnancy losses.
Chaithra, T. P+3 more
core +1 more source
New Catalytic Routes to Benzofused Seven-Membered Azaheterocycles [PDF]
Benzazepines, benzodiazepines and benzoxazepines compose a privileged family of natural products and pharmaceuticals. Their remarkable biological activity made them useful drugs to treat a large variety of issues.
Velasco Rubio, Álvaro
core
Asymmetric deprotonation of N‐benzyl urea derivatives of nitrogen heterocycles leads to enantioselective insertion of the benzylic substituent into an aromatic C−N bond. Treatment of the ring‐expanded products induces a stereospecific ring‐contraction that results in an overall asymmetric enantioselective one‐carbon enlargement of the heterocycle ...
Rajendra K. Mallick+2 more
wiley +2 more sources
Design, Synthesis, and Evaluation of Tetrasubstituted Pyridines as Potent 5-HT2C Receptor Agonists. [PDF]
A series of pyrido[3,4-d]azepines that are potent and selective 5-HT2C receptor agonists is disclosed. Compound 7 (PF-04781340) is identified as a suitable lead owing to good 5-HT2C potency, selectivity over 5-HT2B agonism, and in vitro ADME properties ...
Allwood, Daniel M+11 more
core +4 more sources
Comparative study of dopaminergic activity of tetrahydro-1H-[3]-benzazepines and their precursors [PDF]
The discovery of the tetrahydro-1H-[3]-benzazepine SCH23390 [1], represented one of the most important advances in the study of dopaminergic receptors due to their behavior as a selective D1 receptor antagonist.
Contreras-Cáceres, Rafael+5 more
core