Process for preparing chiral dipeptidyl peptidase-IV inhibitors
US-9187488-B2 · Nov 17, 2015 · US
US10053466B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-10053466-B2 |
| Application number | US-201715831895-A |
| Country | US |
| Kind code | B2 |
| Filing date | Dec 5, 2017 |
| Priority date | Jul 21, 2014 |
| Publication date | Aug 21, 2018 |
| Grant date | Aug 21, 2018 |
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A process for preparing a compound of structural Formula Ia: comprising Boc deprotection with TFA of: and reductive amination of:
Opening claim text (preview).
What is claimed is: 1. A process of preparing a compound of Formula 7 comprising reacting 2,4-difluorobenzaldehyde and nitromethane in the present of a copper salt, ligand, base and solvent to produce a compound of Formula 17: 2. The process of claim 1 further comprising the step of reacting the compound of Formula 17 with acrolein in the presence of a base and solvent to produce a compound of Formula 18: 3. The process of claim 2 further comprising the step of reacting the compound of Formula 18 with a chlorinating agent in the presence of a base and a solvent to produce a compound of Formula 19: 4. The process of claim 3 further comprising the step of crystallizing the compound of Formula 19 under basic conditions to produce a compound of Formula 19t: 5. The process of claim 4 further comprising the steps of reacting the compound of Formula 19t with a hydrobrating agent and an oxidant to produce a compound of Formula 20: and reacting the compound of Formula 20 with a reducing agent and a protecting group to produce a compound of Formula 21:
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