Results 21 to 30 of about 1,536 (171)

One-pot functionalisation of N-substituted tetrahydroisoquinolines by photooxidation and tunable organometallic trapping of iminium intermediates

Beilstein Journal of Organic Chemistry, 2014
Nucleophilic trapping of iminium salts generated via oxidative functionalisation of tertiary amines is well established with stabilised carbon nucleophiles.
Joshua P. Barham, Matthew P. John, John A. Murphy   +2 more
doaj   +1 more source

De Novo Discovery of Nonstandard Thioisoindole‐Bridged Bicyclic Peptides Targeting Traf2‐ and NCK‐Interacting Kinase

Angewandte Chemie, EarlyView.
An optimized strategy for the ribosomal synthesis of thioisoindole‐bridged bicyclic (TiB) peptides is incorporated into the RaPID platform, enabling high‐throughput discovery from topologically defined TiB libraries. Proof‐of‐concept selection against TNIK identifies nanomolar‐affinity ligands with inhibitory activity, while x‐ray crystallography ...
Yue Zhang, Alexander A. Vinogradov, Keisuke Hamada, Yin Sun, Toru Sengoku, Hiroaki Suga   +5 more
wiley   +2 more sources

Direct and Efficient C(sp3)–H Functionalization of N-Acyl/Sulfonyl Tetrahydroisoquinolines (THIQs) With Electron-Rich Nucleophiles via 2,3-Dichloro-5,6-Dicyano-1,4-Benzoquinone (DDQ) Oxidation

Frontiers in Chemistry, 2020
A highly efficient metal-free oxidative direct C(sp3)–H functionalization of N-acyl/sulfonyl 1,2,3,4-tetrahydroisoquinolines (THIQs) with a wide range of electron-rich nucleophiles was accomplished under mild conditions through oxidation with DDQ and ...
Heesun Yu, Hyoungsu Kim, Seung-Hoon Baek, Dongjoo Lee   +3 more
doaj   +1 more source

Iridium‐Catalyzed Ionic Hydrogenation of Multi‐Aza Heterocycles

Angewandte Chemie, EarlyView.
Saturated nitrogen‐containing heterocycles are ubiquitous in bioactive molecules and are thus attractive synthetic targets. A readily accessible cyclometalated iridium(III) complex reduces 14 different aromatic aza heterocycles to (partially)saturated multi aza‐heterocycles enlarging accessible chemical space while displaying high tolerance toward ...
Arthur Despois, Nicolai Cramer
wiley   +2 more sources

Cross-Cyclotrimerization with Two Nitriles as a Synthetic Pathway to Unsymmetrically 3,3’-Disubstituted bis(Tetrahydroisoquinolines)

Molecules, 2009
Microwave assisted CpCo(CO)2 catalyzed cross-cyclotrimerizations of 1,7,9,15-hexadecatetrayne with two different nitriles to give unsymmetrically substituted bis(tetrahydroisoquinolines) was studied.
Aneta Kadlčíková, Martin Kotora
doaj   +1 more source

Borylcyclopropanes: Synthetic Strategies and Applications

Angewandte Chemie, EarlyView.
Borylcyclopropanes (cyclopropanes bearing a boron substituent) sit at the intersection of two privileged frameworks in synthesis. This review provides the first exhaustive survey of their chemistry, spanning metal–carbene, nucleophilic cyclization, radical, hydroboration, and C─H activation routes, and documenting applications in medicinal chemistry ...
Aiza A. Butt, Joseph M. Ready
wiley   +2 more sources

Synthesis of 1-(para-methoxyphenyl)tetrazolyl-Substituted 1,2,3,4-Tetrahydroisoquinolines and Their Transformations Involving Activated Alkynes

Molecules, 2018
1-(p-Methoxyphenyl)tetrazolyl-substituted 6,7-dimethoxy(6,7-methylenedioxy)-1,2,3,4-tetrahydroisoquinolines formed tetrazolyl-substituted azocines in high yields by using activated alkynes.
Alexander A. Titov, Reza Samavati, Elena V. Alexandrova, Tatiana N. Borisova, Tuyet Anh Dang Thi, Van Tuyen Nguyen, Tuan Anh Le, Alexey V. Varlamov, Erik V. Van der Eycken, Leonid G. Voskressensky   +9 more
doaj   +1 more source

Pharmacokinetic Study and Metabolite Identification of 1-(3′-bromophenyl)-heliamine in Rats

Pharmaceuticals, 2022
Tetrahydroisoquinolines have been widely investigated for the treatment of arrhythmias. 1−(3′−bromophenyl)−heliamine (BH), an anti−arrhythmias agent, is a synthetic tetrahydroisoquinoline. This study focuses on the pharmacokinetic characterization of BH,
Ruqi Xi, Rahima Abdulla, Miaomiao Zhang, Zhurakulov Sherzod, Vinogradova Valentina Ivanovna, Maidina Habasi, Yongqiang Liu   +6 more
doaj   +1 more source

Carbon nitride photocatalyzes regioselective aminium radical addition to the carbonyl bond and yields N-fused pyrroles

Nature Communications, 2019
Photochemistry offers new means to perform organic chemistry, although these transformations typically require additives. Here, the authors study reactions between tetrahydroisoquinolines and chalcones under visible light using carbon nitrides for ...
Bogdan Kurpil, Katharina Otte, Artem Mishchenko, Paolo Lamagni, Wojciech Lipiński, Nina Lock, Markus Antonietti, Aleksandr Savateev   +7 more
doaj   +1 more source

Synthesis of C3/C1-Substituted Tetrahydroisoquinolines

Molecules, 2015
A broad biological screening of the natural alkaloid N-methylisosalsoline (2) extracted from Hammada scoparia leaves against a panel of human and parasitic proteases revealed an interesting activity profile of 2 towards human 20S proteasome. This outcome
Mohamed Mihoubi, Nicola Micale, Angela Scala, Raoudha Mezghani Jarraya, Amira Bouaziz, Tanja Schirmeister, Francesco Risitano, Anna Piperno, Giovanni Grassi   +8 more
doaj   +1 more source