38073-22-2

Upstream product

• 117719-66-1 3-(2-aminoethyl)-4-cyanoindole 
• 830-96-6 Indole-3-propionic acid 
• 160320-10-5 1-(2,2-Dimethyl-propionyl)-3,4-dihydro-1H-benzo[cd]indol-5-one 
• 1028267-60-8 3-[1-(2,2-Dimethyl-propionyl)-1H-indol-3-yl]-propionyl chloride 
• 160320-11-6 3-(1-pivaloyl-1H-indol-3-yl)propanoic acid 
• 117719-63-8 4-cyano-3-(2-nitroethyl)indole 
• 117719-60-5 (E)-4-cyano-3-(2-nitrovinyl)indole 
• 39830-66-5 methyl 1H-indole-4-carboxylate 
• 123883-35-2 methyl 3-(2-nitroethyl)-1H-indole-4-carboxylate 

Downstream Products

• 283173-02-4 2-(4-(N-methylamino)methylphenyl)-3,4,5,6-tetrahydro-1H-azepino[5,4,3-cd]indol-6-one 
• 283172-71-4 2-(3-Hydroxymethylphenyl)-3,4,5,6-tetrahydro-1H-azepino[5,4,3-cd]indol-6-one 
• 283172-70-3 2-(3-Nitrophenyl)-3,4,5,6tetrahydro-1H-azepino[5,4,3-cd]indol-6-one 
• 283173-47-7 2-(4-Methanesulfinyl-phenyl)-1,3,4,5-tetrahydro-azepino[5,4,3-cd]indol-6-one 
• 283173-62-6 2-(3-Pyrrolidin-1-ylmethylphenyl)-3,4,5,6-tetrahydro-1H-azepino[5,4,3-cd]indol-6-one 
• 283173-20-6 2-(2-methoxy-phenyl)-1,3,4,5-tetrahydro-azepino[5,4,3-cd]indol-6-one 
• 283172-77-0 8-Bromo-2-phenyl-3,4,5,6-tetrahydro-1H-azepino[5,4,3-cd]indol-6-one 
• 283172-99-6 2-Biphenyl-4-yl-1,3,4,5-tetrahydro-azepino[5,4,3-cd]indol-6-one 
• 283173-17-1 2-(4-chloro-phenyl)-1,3,4,5-tetrahydro-azepino[5,4,3-cd]indol-6-one 
• 283172-95-2 2-(3-chlorophenyl)-1,3,4,5-tetrahydro-azepino[5,4,3-cd]indol-6-one 
• 283172-88-3 2-(4-bromophenyl)-1,3,4,5-tetrahydro-azepino[5,4,3-cd]indol-6-one 
• 283173-13-7 2-(4-hydroxy-phenyl)-1,3,4,5-tetrahydro-azepino[5,4,3-cd]indol-6-one 
• 283173-46-6 2-(4-methylsulfanyl-phenyl)-1,3,4,5-tetrahydro-azepino[5,4,3-cd]indol-6-one 
• 283172-94-1 2-(2,4-difluoro-phenyl)-1,3,4,5-tetrahydro-azepino[5,4,3-cd]indol-6-one 

Relevant academic research and scientific papers

Copper-Mediated Radiosynthesis of [18F]Rucaparib

The poly(ADP-ribose) polymerase (PARP) inhibitor rucaparib is used in the clinic to treat BRCA-mutated cancers. Herein, we report two strategies to access the 18F-isotopologue of rucaparib by applying a copper-mediated nucleophilic 18F-fluorodeboronation. The most successful approach features an aldehydic boronic ester precursor that is subjected to reductive amination post-18F-labeling and affords [18F]rucaparib with an activity yield of 11% ± 3% (n = 3) and a molar activity (Am) up to 30 GBq/μmol. Preliminary in vitro studies are presented.

Substituted indolo azaketone compound and preparation method and application thereof

The invention discloses a substituted indolo azaketone compound or pharmaceutically acceptable salt thereof and a preparation method and application of the substituted indolo azaketone compound. The structure of the compound is shown as (I). The substitut

Poly(ADP-ribose) Polymerase in Neurodegeneration: Radiosynthesis and Radioligand Binding in ARC-SWE tg Mice

We report the synthesis, radiosynthesis, and characterization of a radioligand for poly(ADP-ribose) polymerase (PARP). PARP is of central importance in cell homeostasis, neuroplasticity, and neurodegeneration in the brain. A radiolabeled PARP inhibitor was developed and used for autoradiographic quantification of PARP protein concentration in wild-type and transgenic rodent brains ex vivo in high resolution. The binding of [3H]rucaparib was found to be confined to PARP-expressing domains, for example, cerebellar cortex or hippocampal regions in both models. Saturation binding experiments confirmed selective and reversible binding to a single site (Kd = 1.1 ± 0.2 nM).

TRICYCLIC ISOQUINOLINE DERIVATIVES FOR TREATMENT OF OBESITY

The present invention relates to novel compounds of formula (I): wherein R1, R2, R3, R4, and R5 are as described herein, to pharmaceutical compositions comprising the compounds, to processes for their

Synthesis of analogs of the ergot alkaloids

A number of 3,4,5,6-tetrahydro-1H-azepino[5,4,3-cd]indole derivatives have been synthesized starting with methyl indole-4-carboxylate functionalized at the 3 position.

1,9-Alkano-Bridged 2,3,4,5-Tetrahydro-1H-3-benzazepines with Affinity for the α2-Adrenoceptor and the 5-HT1A Receptor

A number of 1,9-alkano-bridged 2,3,4,5-tetrahydro-1H-3-benzazepines were prepared and evaluated for 5-HT1A receptor and α2-adrenoceptor affinity by using radioligand receptor binding techniques.Several compounds displayed 5-HT1A receptor affinity comparable to, or greater than, the known 5-HT1A ligand buspirone.The highest affinity 5-HT1A receptor ligands were N-alkyl-, N-allyl-5-chloro-, and 5-methoxy-1,2,3,4,8,9,10,10a-octahydronaphthazapines (4c, 4m, 4n), which had pKi values of 7.9-8.1.The S enantiomer of 4c had a higher affinity for the 5-HT1A receptor than the corresponding R isomer (pKi of 8.2 for (S)-4c vs 7.7 for (R)-4c).These compounds had a relatively low affinity for the α2-adrenoceptor (pKi of 7 or less).On the other hand, the closely related 5-chloro-2-methyl-2,3,4,8,9,9a-hexahydro-1H-indenoazepine (3b) had high affinity for both the α2-adrenoceptor (pKi=8.1) and 5-HT1A receptor (pKi=7.6).These results indicate that the two receptors may share common recognition sites.