Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Sulfuric Acid | HCID 1118 | — |
| Reactant | Sitagliptin | HCID 4369359 | — |
| Solvent | Isopropanol | HCID 3776 | — |
| Product | HCID 71724478 | HCID 71724478 | — |
Reaction Steps
Sitagliptin (5 g) and isopropanol (75 mL) are charged into a round-bottom flask and the mixture is heated to about 80° C. for about 15 minutes to obtain a clear dissolution. Sulfuric acid (1.2 g) is added and the reaction mixture is refluxed for about 1 hour. The reaction mixture is cooled to about 30° C. and stirred for about 22 hours. The separated solid is filtered, washed with isopropanol (5 mL), and dried under reduced pressure at about 40° C. for about 1.5 hours to afford the title compound. (Yield: 6.0 g; MC: 0.84% w/w; HPLC purity: 99.98%)
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US08309724B2 |
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| Source dataset | uspto-grants-2012_11 |
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| ORD ID | ord-c5cb5b098f6f43b59e299b5d7585f9ff |
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| Source note | uspto-grants-2012_11 |
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