Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Fumaric Acid | HCID 444972 | — |
| Reactant | Sitagliptin | HCID 4369359 | — |
| Solvent | Isopropanol | HCID 3776 | — |
| Product | HCID 86647030 | HCID 86647030 | — |
Reaction Steps
Sitagliptin (4 g) and isopropanol (60 mL) are charged into a round-bottom flask and the mixture is heated to about 80° C. for about 30 minutes to obtain a clear dissolution. Fumaric acid (1.14 g) is added and the reaction mixture is refluxed for about 2 hours. The reaction mixture is cooled to about 30° C. and stirred for about 21 hours. The separated solid is filtered, washed with isopropanol (4 mL), and dried under reduced pressure at about 45° C. for about 2 hours to afford the title compound. (Yield: 4.0 g; MC: 1.05% w/w; HPLC purity: 99.47%)
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| Patent number | US08309724B2 |
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| Source dataset | uspto-grants-2012_11 |
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| ORD ID | ord-be9e5ff4b7db4341b3a252eb00b87b0e |
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| Source note | uspto-grants-2012_11 |
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