Process for preparing chiral dipeptidyl peptidase-IV inhibitors
US-9187488-B2 · Nov 17, 2015 · US
US9862725B2 · US · B2
| Field | Value |
|---|---|
| Publication number | US-9862725-B2 |
| Application number | US-201515325100-A |
| Country | US |
| Kind code | B2 |
| Filing date | Jul 16, 2015 |
| Priority date | Jul 21, 2014 |
| Publication date | Jan 9, 2018 |
| Grant date | Jan 9, 2018 |
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A process for preparing a compound of structural Formula Ia: comprising Boc deprotection with TFA of, reductive amination of:
Opening claim text (preview).
What is claimed is: 1. A process for preparing a compound of structural Formula Ia: comprising reacting a compound of Formula 1 with TFA: to produce a TFA salt of a compound of Formula 1a: and reacting the TFA salt of a compound of Formula 1a with a compound of Formula 7 under reductive amination conditions: to produce the compound of Formula Ia. 2. The process of claim 1 , wherein the process is done as a through process. 3. The process of claim 1 , further comprising the step of crystallizing Formula Ia. 4. The process of claim 1 , wherein the amount of TFA is 1-5 volumes. 5. The process of claim 1 , wherein the amount of TFA is 3 volumes. 6. A process of preparing a compound of structural Formula I: comprising reacting a compound of Formula 1 with TFA: to produce a TFA salt of a compound of Formula 1a: reacting the TFA salt of a compound of Formula 1a with a compound of Formula 7 under reductive amination conditions: to produce a compound of Formula Ia; and removing the Boc group of Formula Ia to produce the compound of Formula I. 7. The process of claim 6 , wherein the compound of Formula Ia is crystallized prior to removing the Boc protecting group.
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