321840-35-1

Upstream product

• 174770-74-2 (R)-2-amino-2-(4-fluorophenyl)ethanol 
• 74-88-4 methyl iodide 
• 19883-57-9 (S)-2-amino-2-(4-fluorophenyl)acetic acid 
• 93939-74-3 (R)-2-(4-fluorophenyl)glycine 

Downstream Products

• 177948-41-3 1-tert-Butyloxycarbonyl-4-[(R)-1-(4-fluorophenyl)-2-methoxyethyl]aminopiperidine 

Relevant academic research and scientific papers

PYRAZOLE DERIVATIVES AS INHIBITORS OF RECEPTOR TYROSYNE KINASES

Compounds of formula (I): and their use in the inhibition of Trk activity are described.

3-[3-(piperidin-1-yl)propyl]indoles as highly selective h5-HT(1D) receptor agonists

Several 5-HT(ID/1B) receptor agonists are now entering the marketplace as treatments for migraine. This paper describes the development of selective h5-HT(1D)receptor agonists as potential antimigraine agents which may produce fewer side effects. A series of 3-[3-(piperidin-1-yl)propyl]indoles has been synthesized which has led to the identification of 80 (L-772,405), a high- affinity h5-HT(1D) receptor full agonist having 170-fold selectivity for h5- HT(1D) receptors over h5-HT(1B) receptors. L-772,405 also shows very good selectivity over a range of other serotonin and nonserotonin receptors and has excellent bioavailability following subcutaneous administration in rats. It therefore constitutes a valuable tool to delineate the role of h5-HT(1D) receptors in migraine. Molecular modeling and physical properties have been utilized to postulate the binding conformation of these compounds in the receptor cavity.

Azetidine, pyrrolidine and piperidine derivatives

A class of substituted azetidine, pyrrolidine and piperidine derivatives are selective agonists of 5-HT1 -like receptors, being potent agonists of the human 5-HT1Dα receptor subtype whilst possessing at least a 10-fold selective affinity for the 5-HT1Dα receptor subtype relative to the 5-HT1Dβ subtype; they are therefore useful in the treatment and/or prevention of clinical conditions, in particular migraine and associated disorders, for which a subtype-selective agonist of 5-HT1D receptors is indicated, whilst eliciting fewer side-effects, notably adverse cardiovascular events, than those associated with non-subtype-selective 5-HT1D receptor agonists.