Results 71 to 80 of about 32,974 (279)

Electrochemically Driven Regioselective Radical Functionalization of Allenes: Scope and Mechanistic Insights

Advanced Science, EarlyView.
Allenes emerge as powerful platforms for electrochemical functionalization through radical pathways. Selective radical addition at the central carbon triggers anodic oxidation and intramolecular cyclization, enabling efficient synthesis of oxazolines and oxazolidine‐2‐imines without external oxidants.
Pranjal Pyne, Prateek Saini, Rohel Hoque, Shivam Pandey, Srinivasan Ramakrishnan, Chandra M. R. Volla   +5 more
wiley   +1 more source

Breakthrough Design of Highly Potent Antivirals Against Wild‐Type HIV‐1 and Lenacapavir‐Resistant M66I Variant

Angewandte Chemie, EarlyView.
Lenacapavir, the first‐in‐class drug targeting HIV‐1 capsid, is a breakthrough drug in HIV‐1 treatment and prophylaxis. However, a single M66I mutation confers complete viral resistance to lenacapavir. We report herein the design and synthesis of innovative R2 analogs demonstrating low nM potency against HIV‐1 M66I and excellent pharmacokinetics in ...
Nicolas Jamey, D. M. Nirosh Udayanga, Huanchun Zhang, Roshan Katekar, Wei Xie, Shreya M. Ravichandran, Xinyong Cai, Zachary C. Lorson, William M. McFadden, Won Hee Ryu, Jiashu Xie, Karen A. Kirby, Stefan G. Sarafianos, Zhengqiang Wang   +13 more
wiley   +2 more sources

Cobalt‐Catalyzed Asymmetric Construction of Boron Stereocenters With C–N Axial Chirality

Advanced Science, EarlyView.
A cobalt/Salox‐catalyzed one‐pot annulation enables enantioselective formation of B‐stereogenic centers and C─N axial chirality via C─H/N─H annulation, affording diverse fluorescent products with high stereocontrol and optoelectronic potential. ABSTRACT The efficient construction of boron stereogenic centers alongside axial chirality remains a ...
Subramani Kumaran, Harihara Subramanian Ravi Sankar, Pritam Maity, J. Richard Premkumar, Abir Das, Basker Sundararaju   +5 more
wiley   +1 more source

Direct Access to Chiral Piperidines by Enantioselective HAT‐Initiated C(sp3)─H Oxidation

Angewandte Chemie, EarlyView.
The direct desymmetrization of piperidines is achieved through manganese‐catalyzed enantioselective α‐C(sp3)─H oxidation with hydrogen peroxide, affording versatile chiral N,O‐acetals in good yields and with high enantio‐ and diastereoselectivity. These intermediates provide access to diverse functionalized piperidines with retention of chirality ...
Sethuraman Muthuramalingam, Josep M. Luis, Arnau Call, Quentin Lefebvre, Matthew S. Sigman, Miquel Costas   +5 more
wiley   +2 more sources

Exploring the Phe-Gly Dipeptide-Derived Piperazinone Scaffold in the Search for Antagonists of the Thrombin Receptor PAR1

Molecules, 2014
A series of Phe-Gly dipeptide-derived piperazinones containing an aromatic urea moiety and a basic amino acid has been synthesized and evaluated as inhibitors of human platelet aggregation induced by the PAR1 agonist SFLLRN and as cytotoxic agents in ...
Ángel M. Valdivielso, M. Teresa García-López, Marta Gutiérrez-Rodríguez, Rosario Herranz   +3 more
doaj   +1 more source

Ziegler–Natta Catalysts: Regioselectivity and “Hydrogen Response”

, 2019
Advanced High Throughput Experimentation (HTE) methods were applied to quantify the regioselectivity and the so-called “hydrogen response” in propene polymerization of four Ziegler–Natta catalysts representative of the three latest industrial ...
Nic. Friederichs (2533612), Roberta Cipullo, Anika Meppelder (4093591), Antonio Vittoria, Anika Meppelder, Roberta Cipullo (2081539), Antonio Vittoria (4093588), Vincenzo Busico (1880728), Vincenzo Busico, Nic. Friederichs   +9 more
core   +1 more source

NiH‐Catalyzed Enantio‐ and Regioselective Hydroselenylation of Unactivated Alkenes

Advanced Science, EarlyView.
Nickel‐hydride‐catalyzed enantio‐ and regioselective hydroselenylation of unactivated alkenes provides access to chiral organoselenium compounds. Enantiodetermining Ni–H insertion followed by single‐electron diselenide activation generates selenyl radical.
Hyung‐Joon Kang, Jaehun Kim, Sungwoo Hong   +2 more
wiley   +1 more source

A de‐novo Approach Towards Divergent [3+2π/σ] Photocycloadditions of Nitrones via Assembly‐Controlled Kinetic Electron Transfer Gating

Angewandte Chemie, EarlyView.
A metal‐free photocatalytic platform converts nitrones into 4‐isoxazolines and oxa–aza–bicycloheptanes through divergent [3+2π/σ] cycloadditions. Assembly‐controlled kinetic electron transfer gating dictates substrate activation, enabling selective reactivity beyond thermodynamic expectations.
Nayan Saha, Rajesh Kancherla, Jorge Escorihuela, Shana Chandran, Mrinal K. Bera, Magnus Rueping, Burkhard König   +6 more
wiley   +2 more sources

Theoretical Study on Regioselectivity of the Diels-Alder Reaction between 1,8-Dichloroanthracene and Acrolein

Molecules, 2016
A theoretical study of the regioselectivity of the Diels-Alder reaction between 1,8-dichloroanthracene and acrolein is performed using DFT at the B3LYP/6-31G(d,p) level of theory.
Mujeeb A. Sultan, Usama Karama, Abdulrahman I. Almansour, Saied M. Soliman   +3 more
doaj   +1 more source

A Small‐Molecule DEPTAC Rescues Cognitive Deficits by Targeted Dephosphorylation of Pathological Tau

Advanced Science, EarlyView.
TP2 is a fully synthetic small‐molecule dephosphorylation‐targeting chimera that recruits endogenous PP2A‐Bα to Tau, enabling targeted removal of pathological phosphate modifications. In two tauopathy mouse models, systemic TP2 reduces Tau pathology, preserves neuronal and synaptic integrity, improves neuroimmune homeostasis, and rescues cognition ...
Fei Sun, Yang Liu, Qiuzhi Zhou, Qingyuan Hu, Weixia Wang, Yue Xiao, Jingfen Su, Guanting Liu, Miaomiao Sun, Lixia Chen, Hua Li, Ying Yang, Jian‐Zhi Wang   +12 more
wiley   +1 more source