59496-25-2Relevant articles and documents
A flexible, convergent approach to polycyclic indole structures: Formal synthesis of (±)-mersicarpine
Blechy, Aurellen,Zard, Samir Z.
, p. 2800 - 2803 (2009)
The formal synthesis of (±)-mersicarpine was achieved using an lntermolecular radical addition-radical cyclization cascade. This key reaction represents a flexible, convergent route to numerous polycyclic indole derivatives.
Synthesis and Pharmacological Profiling of the Metabolites of Synthetic Cannabinoid Drugs APICA, STS-135, ADB-PINACA, and 5F-ADB-PINACA
Longworth, Mitchell,Connor, Mark,Banister, Samuel D.,Kassiou, Michael
, p. 1673 - 1680 (2017)
Synthetic cannabinoids (SCs) containing a 1-pentyl-1-H substituted indole or indazole are abused around the world and are associated with an array of serious side effects. These compounds undergo extensive phase 1 metabolism after ingestion with little understanding whether these metabolites are contributing to the cannabimimetic activity of the drugs. This work presents the synthesis and pharmacological characterization of the major metabolites of two high concern SCs; APICA and ADB-PINACA. In a fluorometric assay of membrane potential, all metabolites that did not contain a carboxylic acid functionality retained potent activity at both the CB1 (EC50 = 14-787 nM) and CB2 (EC50 = 5.5-291 nM) receptors regardless of heterocyclic core or 3-carboxamide substituent. Of note were the 5-hydroxypentyl and 4-pentanone metabolites which showed significant increases in CB2 functional selectivity. These results suggest that the metabolites of SCs potentially contribute to the overall pharmacological profile of these drugs.
Palladium-Catalyzed Silacyclization of (Hetero)Arenes with a Tetrasilane Reagent through Twofold C?H Activation
Wang, Dingyi,Li, Mingjie,Chen, Xiangyang,Wang, Minyan,Liang, Yong,Zhao, Yue,Houk, Kendall N.,Shi, Zhuangzhi
supporting information, p. 7066 - 7071 (2021/03/01)
The use of an operationally convenient and stable silicon reagent (octamethyl-1,4-dioxacyclohexasilane, ODCS) for the selective silacyclization of (hetero)arenes via twofold C?H activation is reported. This method is compatible with N-containing heteroarenes such as indoles and carbazoles of varying complexity. The ODCS reagent can also be utilized for silacyclization of other types of substrates, including tertiary phosphines and aryl halides. A series of mechanistic experiments and density functional theory (DFT) calculations were used to investigate the preferred pathway for this twofold C?H activation process.
Indole derivative as well as preparation method and application thereof
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Paragraph 0063-0065, (2021/06/23)
The invention discloses an indole derivative as well as a preparation method and application thereof, belongs to the technical field of medicines, and particularly relates to an indole derivative as shown in a general formula I, the invention also relates
