110331-29-8

Upstream product

• 110-89-4 piperidine 
• 221284-00-0 2-bromo-3-[2-(tetrahydro-2H-pyran-2-yloxy)ethyl]-1H-indole 
• 98-80-6 phenylboronic acid 
• 147375-18-6 2-(2-phenyl-1H-indol-3-yl)-1-(piperidin-1-yl)ethan-1-one 
• 5882-82-6 (E)-1-(3-phenylallyl)piperidine 
• 201230-82-2 carbon monoxide 
• 100-63-0 phenylhydrazine 
• 116576-38-6 3-o-nitrophenyl-1-(N-piperidinyl)-2-propen-1-one 
• 100-52-7 benzaldehyde 
• 58106-56-2 ethyl (E)-3-(2-aminophenyl)acrylate 
• 4567-06-0 (2-phenyl-1H-indol-3-yl)acetic acid ethyl ester 
• 10229-11-5 4-phenyl-but-3-yn-1-ol 
• 59-88-1 phenylhydrazine hydrochloride 
• 92962-52-2 2-(2-phenyl-1H-indol-3-yl)ethan-1-ol 

Relevant academic research and scientific papers

Solid-phase synthesis of 2,3-disubstituted indoles: Discovery of a novel, high-affinity, selective h5-HT(2A) antagonist

The application of a novel solid-phase synthesis of 2,3-disubstituted indoles utilizing a carbamate indole linker is described resulting in the identification of the novel, high-affinity, selective h5-HT(2A) antagonist 19. (C) 2000 Elsevier Science Ltd.

N-Heterocyclic-Carbene-Catalyzed Umpolung of Imines

N-Heterocyclic carbene (NHC) catalysis has been widely used for the umpolung of aldehydes, and recently for the umpolung of Michael acceptors. Described herein is the umpolung of aldimines catalyzed by NHCs, and the reaction likely proceeds via aza-Breslo

Rhodium(III)-catalyzed c-h activation and indole synthesis with hydrazone as an auto-formed and auto-cleavable directing group

An efficient, practical, and external-oxidant-free indole synthesis from readily available aryl hydrazines was developed, by using hydrazone as a directing group for RhIII-catalyzed C-H activation and alkyne annulation. The hydrazone group was formed by in situ condensation of hydrazines and Ci￡O source, whereas its N-N bond was served as an internal oxidant, for which we termed it as an auto-formed and auto-cleavable directing group (DGauto). This method needs no step for pre-installation and post-cleavage of the directing group, making it a quite easily scalable approach to access unprotected indoles with high step economy. The DGauto strategy was also applicable for isoquinoline synthesis. In addition, synthetic utilities of this chemistry for rapid assembly of π-extended nitrogen-doped polyheterocycles and bioactive molecules were demonstrated. Copyright

Preparation of indoles from α-aminonitriles: A short synthesis of FGIN-1-27

α-Aminonitriles derived from 2-aminocinnamic acid esters and amides can be cyclized under basic conditions to furnish substituted indole-3-acetic acid derivatives in quantitative yield. The reaction provides a simple access to a class of biologically acti

2,3-Disubstituted indoles from olefins and hydrazines via tandem hydroformylation-Fischer indole synthesis and skeletal rearrangement

The tandem hydroformylation-Fischer indolisation protocol is used in the synthesis of 2,3-disubstituted indoles. After hydroformylation of selected olefins to form α-branched aldehydes in a one-pot procedure these are condensed with phenylhydrazine to give hydrazones. Upon acid-promoted [3,3]-sigmatropic rearrangement indolenine intermediates with quaternary centres in the 3-position are formed, which, after selective Wagner-Meerwein-type rearrangement of one of the substituents from the 3- to the 2-position, lead to 2,3-disubstituted indoles. Several olefins, bearing substituents with various functional groups, as well as cyclic olefinic systems are investigated. The Royal Society of Chemistry 2006.

Phenylindole derivatives as 5-HT2A receptor ligands

A class of tryptamine analogues bearing an optionally substituted phenyl nucleus at the 2-position are selective antagonists of the human 5-HT2Areceptor and are therefore useful as pharmaceutical agents, especially in the treatment and/or preve

2-aryl tryptamines: Selective high-affinity antagonists for the h5-HT(2A) receptor

A series of 2-aryl tryptamines have been identified as high-affinity h5-HT(2A) antagonists. Structure-activity relationship studies have shown that h5-HT(2A) affinity can be attained via modifications to the tryptamine side chain and that selectivity over h5-HT(2C) and hD2 receptors can be controlled by suitable C-2 aryl groups. (C) 2000 Elsevier Science Ltd.