- Rhodium(III)-catalyzed selective C-H cyanation of indolines and indoles with an easily accessible cyano source
-
The rhodium-catalyzed selective cyanation of C-H bonds of indolines and indoles with N-cyano-N-phenyl-para-methylbenzenesulfonamide is described. This protocol offers a facile access to C-7 cyanated indolines and C-2 cyanated indoles with high site selectivity and excellent functional group tolerance.
- Mishra, Neeraj Kumar,Jeong, Taejoo,Sharma, Satyasheel,Shin, Youngmi,Han, Sangil,Park, Jihye,Oh, Joa Sub,Kwak, Jong Hwan,Jung, Young Hoon,Kim, In Su
-
-
Read Online
- Indoline Catalyzed Acylhydrazone/Oxime Condensation under Neutral Aqueous Conditions
-
Acylhydrazones formation has been widely applied in materials science and biolabeling. However, their sluggish condensation rate under neutral conditions limits its application. Herein, indolines with electron-donating groups are reported as a new catalyst scaffold, which can catalyze acylhydrazone, hydrazone, and oxime formation via an iminium ion intermediate. This new type of catalyst showed up to 15-fold rate enhancement over the traditional anilinecatalyzed reaction at neutral conditions. The identified indoline catalyst was successfully applied in hydrogel formation.
- Zhou, Yuntao,Piergentili, Irene,Hong, Jennifer,Helm, Michelle P. Van Der,MacChione, Mariano,Li, Yao,Eelkema, Rienk,Luo, Sanzhong
-
supporting information
p. 6035 - 6040
(2020/10/02)
-
- INSECTICIDAL AMIDES WITH NITROGEN-CONTAINING BENZO-FUSED BICYCLIC RING SYSTEMS
-
Disclosed are compounds of Formula I and compounds of Formula II (including all geometric and stereoisomers), N-oxides thereof and salts thereof, certain compositions comprising the compounds of Formula I and/or the compounds of Formula II and certain use
- -
-
-
- Synthesis and evaluation of heterocyclic carboxamides as potential antipsychotic agents
-
Heterocyclic analogues of 1192U90, 2-amino-N-(4-(4-(1,2-benzisothiazol- 3-yl)-1-piperazinyl)-butyl)benzamide hydrochloride (1), were prepared and evaluated as potential antipsychotic agents. These analogues were evaluated in vitro for their binding to the dopamine D2, serotonin 5-HT2, and serotonin 5-HT(1a) receptors and in vivo for their ability to antagonize the apomorphine-induced climbing response in mice. Nine different types of heterocyclic carboxamides were studied in this investigation (i.e., pyridine- , thiophene-, benzothiophene-, quinoline-, 1,2,3,4-tetrahydroquinoline-, 2,3- dihydroindole-, indole-, benzimidazole-, and indazolecarbox-amides). Two derivatives exhibited potent in vivo activities comparable to 1: 3-amino-N- (4(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)butyl)-2-pyridinecarboxamide (16) and 3-amino-N-(4(4-(1,2-benzisothiazol-3-yl)-1-piperazinyl)butyl)-2- thiophenecarboxamide (29). Furthermore, these derivatives were found to be much less active in behavioral models predictive of extrapyramidal side effects than in the mouse climbing assay, which predicts antipsychotic activity. Carboxamides 16 and 29 were selected for further evaluation as potential backup compounds to 1.
- Norman, Mark H.,Navas III, Frank,Thompson, James B.,Rigdon, Greg C.
-
p. 4692 - 4703
(2007/10/03)
-
- Tricyclic compounds
-
Tricyclo benzodiazepines are cholecystokinin antagonists.
- -
-
-
- -
-
The synthesis of three trisubstitued aryloxazolines, 7, 8, and 10, containing an o-methoxyl group served as useful precursors to eight benzo-fused ring systems.In this fashion, novel syntheses for tetralins, indans, chromans, benzofurans, indolines, tetra
- Meyers, A. I.,Reuman, Michael,Gabel, Richard A.
-
p. 783 - 788
(2007/10/02)
-
- 7-(α-Acetylbenzyl)indoline
-
The preparation of compounds of the formula SPC1 Wherein R is selected from the group consisting of hydrogen and chlorine is described. The compounds are useful as chemical intermediates and as anti-inflammatory agents.
- -
-
-