110808-69-0Relevant articles and documents
Total synthesis of RS-42358 and analogs using lateral lithiation
Kowalczyk, Bruce A.
, p. 1113 - 1116 (2000)
A short synthesis of the 5-HT3 receptor antagonist RS-42358 was developed based on the condensation of lactone 2 with S-3- aminoquinuclidine. The position 2 analogs of RS-42358 were made by condensing various primary amines with lactone 2. The key step in the synthesis of lactone 2 was lateral lithiation of diethyl amide 7 using n-BuLi in THF.
Towards a TREK-1/2 (TWIK-Related K+ Channel 1 and 2) dual activator tool compound: Multi-dimensional optimization of BL-1249
Iwaki, Yuzo,Yashiro, Kentaro,Kokubo, Masaya,Mori, Takahiro,Wieting, Joshua M.,McGowan, Kevin M.,Bridges, Thomas M.,Engers, Darren W.,Denton, Jerod S.,Kurata, Haruto,Lindsley, Craig W.
, p. 1601 - 1604 (2019)
This letter describes a focused, multi-dimensional optimization campaign around BL-1249, a fenamate class non-steroidal anti-inflammatory and a known activator of the K2P potassium channels TREK-1 (K2P2.1) and TREK-2 (K2P1
N-Heterocyclic-Carbene-Catalyzed C–H Acylation via Radical Relay
Liu, Shiwen,Man, Yunquan,Xu, Bo,Zeng, Xiaojun
supporting information, p. 944 - 948 (2022/02/05)
A method of N-fluorocarboxamide-directed N-heterocyclic-carbene (NHC)-catalyzed benzylic C–H acylation with aldehydes via the hydrogen atom transfer strategy is disclosed. This transformation involves a sequence of single-electron transfer, 1,5-hydrogen a
Facile Synthesis of Alkylidene Phthalides by Rhodium-Catalyzed Domino C?H Acylation/Annulation of Benzamides with Aliphatic Carboxylic Acids
Liu, Sien,He, Bangyue,Li, Hongyi,Zhang, Xiaofeng,Shang, Yaping,Su, Weiping
supporting information, p. 15628 - 15633 (2021/10/05)
The Rh-catalyzed ortho-C(sp2)?H functionalization of 8-aminoquinoline-derived benzamides with aliphatic acyl fluorides generated in situ from the corresponding acids has been developed. This reaction initiated with 8-aminoquinoline-directed ortho-C(sp2)?H acylation, which was accompanied by subsequent intramolecular nucleophilic acyl substitution of amide group to produce alkylidene phthalides This approach exhibits high stereo-selectivity for Z-isomer products, and tolerates a variety of functional groups as well as aliphatic carboxylic acids with diverse structural scaffolds.
Heterocyclic compound and preparation and application thereof
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Paragraph 0294-0296, (2020/07/24)
The invention relates to bromodomain inhibitors, and provides a compound represented by a general formula I, a pharmaceutically acceptable salt, an enantiomer, a diastereoisomer, an atropisomer, a racemate, a polymorph, a solvate or an isotope-labeled compound (including deuterium substitution) thereof, a preparation method thereof, a pharmaceutical composition containing the same, and applicationthereof in pharmacy.
Rh-Catalyzed annulations of: N -methoxybenzamides with ketenimines: Synthesis of 3-aminoisoindolinones and 3-diarylmethyleneisoindolinones with strong aggregation induced emission properties
Zhou, Xiaorong,Peng, Zhixing,Zhao, Hongyang,Zhang, Zhiyin,Lu, Ping,Wang, Yanguang
supporting information, p. 10676 - 10679 (2016/09/02)
Rhodium-catalyzed C-H activation/annulation reactions of ketenimines with N-methoxybenzamides furnished 3-aminoisoindolin-1-ones and 3-(diarylmethylene)isoindolin-1-ones. The synthesized 3-(diarylmethylene)isoindolin-1-ones exhibited aggregation induced emissions in aqueous tetrahydrofuran solution and strong green-yellow emissions in solids.
PROCESSES FOR THE PREPARATION OF PALONOSETRON
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Page/Page column 14, (2011/02/24)
The present invention relates to novel processes for the preparation of N-[(3S)-1- azabicyclo[2.2.2]oct-3-yl]-5,6,7,8-tetrahydronaphthalene-1-carboxamide of Formula I. The present invention further relates to processes for the preparation of palonosetron or its salts thereof using N-[(3S)-1-azabicyclo[2.2.2]oct-3-yl]-5,6,7,8- tetrahydronaphthalene-1-carboxamide of Formula I as an intermediate.
PREPARATION OF CRYSTALLINE PALONOSETRON HYDROCHLORIDE
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Page/Page column 21, (2010/06/15)
Processes for the preparation of palonosetron hydrochloride and its crystalline forms.
Processes for preparing palonosetron salts
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Page/Page column 10, (2008/12/08)
The present invention provides processes for preparing Palonosetron salts, especially, the hydrochloride salt and intermediates used to prepare Palonosetron salts.
SUBSTITUTED BENZOYLAMINO-INDAN-2-CARBOXYLIC ACIDS AND RELATED COMPOUNDS
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Page/Page column 66-67, (2009/01/24)
The present invention relates to A compound of the formula Ia wherein in any of its stereoisomers forms or a mixture of stereoisomeric forms in any ratio, or a physiologically acceptable salt thereof, wherein the substituents are as described herein. The inventive compounds have CXCR5 inhibitory activity are particularly useful in treating or preventing various inflammatory diseases, such as rheumatoid arthritis, multiple sclerosis, lupus, Crohn's Disease, associated with the modulation of the human CXCR5 receptor.
