84807-08-9

Upstream product

• 52488-36-5 4-bromo-1H-indole 
• 90481-72-4 4-bromo-1-[(4-methylphenyl)sulfonyl]-1H-indole 
• 1258408-23-9 benzyl 4-[1-(toluene-4-sulfonyl)-1H-indol-4-yl]-piperazine-1-carboxylate 
• 255714-24-0 4-piperazin-1-yl-1H-indole dihydrochloride 
• 501-53-1 benzyl chloroformate 

Downstream Products

• 1258408-24-0 benzyl 4-(3-formyl-1H-indol-4-yl)-piperazine-1-carboxylate 
• 1258408-30-8 benzyl 4-(5-formyl-1H-indol-4-yl)-piperazine-1-carboxylate 
• 1258408-34-2 benzyl 6a,7,9,10-tetrahydro-4H-pyrazino[1,2-a]pyrrolo[4,3,2-de]quinoline-8(6H)-carboxylate 
• 1258408-31-9 benzyl 4-(5-formyl-1-tosyl-1H-indol-4-yl)piperazine-1-carboxylate 

Relevant academic research and scientific papers

Novel Aza-analogous ergoline derived scaffolds as potent serotonin 5-HT6 and dopamine D2 receptor ligands.

By introducing distal substituents on a tetracyclic scaffold resembling the ergoline structure, two series of analogues were achieved exhibiting subnanomolar receptor binding affinities for the dopamine D2 and serotonin 5-HT6 receptor subtype, respectively. While the 5-HT 6 ligands were antagonists, the D2 ligands displayed intrinsic activities ranging from full agonism to partial agonism with low intrinsic activity. These structures could potentially be interesting for treatment of neurological diseases such as schizophrenia, Parkinson's disease, and cognitive deficits.

NOVEL 4-(ARYL-4-SULFONYL)-6,6a,7,8,9,10-HEXAHYDRO-4H-4,8,10a-TRIAZA-ACEPHENANTHRYLENE AND 3-ARYLSULFONYL-6,6a,7,8,9,10-HEXAHYDRO-3H-3,8,10a-TRIAZA-CYCLOPENTA[C]FLUORENE DERIVATIVES AS SEROTONIN 5-HT6 LIGANDS

This invention is directed to compounds of formula I or II, which are serotonin 5-HT 6 ligands. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I or II, or a pharmaceutically acceptable salt thereof. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I or II, or a pharmaceutically acceptable salt thereof. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I or II, or a pharmaceutically acceptable salt thereof.

NOVEL 6,6A,7,8,9,10-HEXAHYDRO-4H-4,8,10A-TRIAZA-ACEPHENANTHRYLENE DERIVATIVES AS DOPAMINE D2 LIGANDS

This invention is directed to compounds, which are dopamine D2 ligands. The invention provides a pharmaceutical composition comprising a therapeutically effective amount of a compound of the invention and a pharmaceutically acceptable carrier. The present invention also provides processes for the preparation of the compounds of formula I or formula II, or a pharmaceutically acceptable salt thereof. The present invention further provides a method of treating a subject suffering from a neurodegenerative disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I or formula II, or a pharmaceutically acceptable salt thereof. The present invention further provides a method of treating a subject suffering from a psychiatric disorder comprising administering to the subject a therapeutically effective amount of a compound of formula I or formula II, or a pharmaceutically acceptable salt thereof.

Syntheses of aza-analogous iso-ergoline scaffolds using carbene mediated C-H insertion

A novel direct, flexible, and robust approach to the iso-ergoline tetracyclic system in which a five or six-membered ring is established by intramolecular carbene C-H insertion is reported. The protocol involves a two step conversion of an aromatic aldehyde to the corresponding hydrazone and without purification further conversion to the diazo-compound followed by thermal carbene formation and C-H insertion α to a nitrogen.