HuagongsheHuagongshe Chemistry Print Report · For research reference only
Trichloroacetic Acid → Bisegliptin
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Trichloroacetic Acid | HCID 6421 | — |
| Reactant | Trifluoroacetic anhydride | HCID 9845 | — |
| Reactant | (2S,4S)-1-[2-[(4-ethoxycarbonylbicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carboxamide | HCID 46854534 | — |
| Product | Bisegliptin | HCID 11688894 | 75% |
Reaction Steps
Using (2S,4S)-1-[2-[(4-ethoxycarbonylbicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carboxamide (739 mg), trifluoroacetic anhydride (0.29 mL) as a dehydrating agent and trichloroacetic acid (327 mg) as an acid, a white powder of (2S,4S)-1-[2-[(4-ethoxycarbonylbicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile was obtained (obtained amount: 524 mg, yield: 75%) by the same method of Example 1.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08143427B2 |
| Source dataset | uspto-grants-2012_03 |
| ORD ID | ord-d7f50257a48b47b484d37c463085c658 |
| Source note | uspto-grants-2012_03 |