Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Acetaldehyde | HCID 177 | — |
| Reactant | Acetonitrile | HCID 6342 | — |
| Reactant | Sodium cyanoborohydride | HCID 5003444 | — |
| Reactant | HCID 68411742 | HCID 68411742 | — |
| Solvent | Acetic Acid | HCID 176 | — |
| Product | HCID 59620346 | HCID 59620346 | — |
Reaction Steps
tert-Butyl 1-((2R)-1-(8-amino-2-oxo-1-(pyridin-2-ylmethyl)-1,2,3,4-tetrahydroquinolin-3-ylamino)-4-methyl-1-oxopentan-2-ylamino)-2-methyl-1-oxopropan-2-ylcarbamate (59 mg) and acetaldehyde (29 μL) were sequentially added to acetonitrile (730 μL), and sodium cyanoborohydride (7 mg) and acetic acid (18 μL) were added to the mixture under cooling on ice, followed by stirring for 5 minutes. The resultant mixture was extracted with ethyl acetate and saturated aqueous sodium bicarbonate solution, and the aqueous layer was further extracted with ethyl acetate. The organic layers were combined, and the combined organic layer was washed with saturated aqueous sodium chloride solution, followed by drying over sodium sulfate. The solvent was evaporated under reduced pressure, and the thus-recovered residue was purified through silica gel column chromatography (hexane:ethyl acetate=1:1), whereby the title compound (58 mg) was yielded.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US08501772B2 |
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| Source dataset | uspto-grants-2013_08 |
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| ORD ID | ord-a99a27bb1e7d4eadaaad4fd09b4dbe03 |
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| Source note | uspto-grants-2013_08 |
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