293744-31-7

Upstream product

• 100-39-0 benzyl bromide 
• 293744-26-0 tert-butyl 4-{[(2-bromophenyl)amino]carbonyl}piperidine-1-carboxylate 
• 615-36-1 2-bromoaniline 
• 280115-99-3 tert-butyl 4-(chlorocarbonyl)-piperidine-1-carboxylate 
• 84358-13-4 N-[(tert-butoxy)carbonyl]piperidine-4-carboxylic acid 
• 100-52-7 benzaldehyde 
• 15110-95-9 N-benzylidene-2-bromobenzenamine 
• 100-44-7 benzyl chloride 
• 71687-81-5 N-benzyl-2-bromoaniline 

Downstream Products

• 252882-60-3 tert-butyl 2-oxo-1,2-dihydro-1'H-spiro[indole-3,4-piperidine]-1'-carboxylate 
• 293744-34-0 tert-butyl 1-benzyl-1,2-dihydro-2-oxospiro[3H-indole-3,4'-piperidine]-1'-carboxylate 

Relevant academic research and scientific papers

PYRIDYL PIPERIDINES

The invention provides novel substituted pyridyl piperidine compounds according to Formula (I) which are Wnt pathway inhibitors, their manufacture and use for the treatment of hyperproliferative diseases such as cancer, inflammatory or degenerative diseases.

ANTAGONISTS OF PGD2 RECEPTORS

Described herein are compounds and pharmaceutical compositions containing such compounds that antagonize the PGD2 activated chemoattractant receptor-homologous molecule expressed on TH2 cells (CRTH2). Also described herein are methods of using such CRTH2 antagonists, alone and in combination with other compounds, for treating respiratory, cardiovascular, and other PGD2-dependent or PGD2 mediated conditions or diseases.

Novel 3-spirocyclic indolyl derivatives useful as ORL-1 receptor modulators

The present invention is directed to novel 3-spirocyclic indolyl derivatives, pharmaceutical compositions containing them and their use in the treatment of disorders and conditions modulated by the ORL-1 receptor.

FUSED AND SPIROCYCLE COMPOUNDS AND THE USE THEREOF

The invention relates to fused and spirocycle compounds of Formula (I), or a pharmaceutically acceptable salt, prodrug, or solvate thereof, wherein R1, R2, Q1-Q3, and Z are defined as set forth in the specification. The invention is also directed to the use of compounds of Formula (I) to treat, prevent or ameliorate a disorder responsive to the blockade of calcium channels, and particularly N-type calcium channels. Compounds of the present invention are especially useful for treating pain.

A convenient synthetic route to spiro[indole-3,4'-piperidin]-2-ones

Starting from 1-[(tert-butoxy)carbonyl]piperidine-4-carboxylic acid and 2-bromoaniline, the spiro[indole-3,4'-piperidin]-2-one system was obtained in three high-yielding steps: anilide formation, N(1)-protection, and intramolecular cyclization under Pd catalysis as the key reaction. The preparation of the corresponding 2-bromoanilide was studied. In extension, the same sequence was developed with 4-methyl- and 4-nitro-2-bromoaniline. In the key step, the NO2 group led to a rather diminished yield. The transformation of the protected spiro[indole-3,4'-piperidin]-2'one to the corresponding unprotected dihydroindoles is discussed.