1375471-12-7

Upstream product

• 24424-99-5 di-tert-butyl dicarbonate 
• 1456803-29-4 isopropyl (2S)-2-(tert-butoxycarbonylamino)-3-(methylsulfonyloxy)propanoate 
• 367-23-7 1,2,4-trifluorobenzene 
• 1231932-49-2 2,3,6-trifluorophenylacetyl chloride 
• 114152-23-7 2-(2,3,6-trifluorophenyl)acetic acid 
• 6226-25-1 2,2,2-trifluoroethyl trifluoromethanesulphonate 

Downstream Products

• 1375471-14-9 (3S,5S,6R)-3-amino-6-methyl-1-(2,2,2-trifluoroethyl)-5-(2,3,6-trifluorophenyl)piperidin-2-one hydrochloride 
• 1401066-09-8 (6S)-3'-methyl-N-[(3S,5S,6R)-6-methyl-2-oxo-1-(2,2,2-trifluoroethyl)-5-(2,3,6-trifluorophenyl)piperidin-3-yl]-2',5'-dioxo-5,7-dihydrospiro[cyclopenta[b]pyridine-6,4'-imidazolidine]-3-carboxamide 
• 1401065-96-0 (6R)-3'-methyl-N-[(3S,5S,6R)-6-methyl-2-oxo-1-(2,2,2-trifluoroethyl)-5-(2,3,6-trifluorophenyl)piperidin-3-yl]-2',5'-dioxo-5,7-dihydrospiro[cyclopenta[b]pyridine-6,4'-imidazolidine]-3-carboxamide 

Relevant academic research and scientific papers

Piperidinone carboxamide indane CGRP receptor antagonists

The present invention is directed to piperidinone carboxamide indane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

PROCESS FOR MAKING CGRP RECEPTOR ANTAGONISTS

The disclosure encompasses a novel process for making piperidinone carboxamide indane and azainane derivatives, having less steps and improved yields as compared to previous synthetic methods for making these compounds, which are CGRP receptor antagonists, useful for the treatment of migrane. Conditions for an amide bond formation between an acid and amine include for example reacting the compounds of Formulae B (after salt break) and C with an amide coupling reagent and optionally an additive and an acid and/or a base in a non-reactive solvent.

PIPERIDINONE CARBOXAMIDE SPIROHYDANTOIN CGRP RECEPTOR ANTAGONISTS

The present invention is directed to piperidinone carboxamide spirohydantoin derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

PIPERIDINONE CARBOXAMIDE AZAINDANE CGRP RECEPTOR ANTAGONISTS

The present invention is directed to piperidinone carboxamide azaindane derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also directed to pharmaceutical compositions comprising these compounds and the use of these compounds and compositions in the prevention or treatment of such diseases in which CGRP is involved.

PIPERIDINE CARBOXAMIDE SPIROHYDANTOIN CGRP RECEPTOR ANTAGONISTS

The present invention is directed to piperidinone carboxamide spirohydantoin derivatives which are antagonists of CGRP receptors and useful in the treatment or prevention of diseases in which the CGRP is involved, such as migraine. The invention is also d