Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Hydrochloric Acid | HCID 313 | — |
| Reactant | Sodium Hydroxide | HCID 14798 | — |
| Reactant | Sodium borohydride | HCID 4311764 | — |
| Reactant | HCID 22673287 | HCID 22673287 | — |
| Solvent | Water | HCID 962 | — |
| Solvent | (+-)-2-Butanol | HCID 6568 | — |
| Product | HCID 22673290 | HCID 22673290 | 73.9% |
Reaction Steps
9 g of (±)-2-isobutyryl-2-azabicyclo[2.2.1]hept-5-en-3-one were dissolved in water (32 ml) and 2-butanol (84 ml) under nitrogen and cooled to 0° C. 1.37 g of sodium borohydride were added in portions over the course of 3.5 h. The mixture was stirred for a further 3 h at 20° C., and it was then adjusted to pH 2.5 with a mixture of conc. hydrochloric acid and water (1/1) and then neutralized with 2N NaOH. The solution was evaporated to 40 g. The residue was extracted with 3×80 ml of dichloromethane. The combined organic phases were completely evaporated. The resulting solid was crystallized in 25 ml of toluene. 6.8 g of title compound were obtained. The yield was 73.6%.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| Patent number | US06252112B1 |
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| Source dataset | uspto-grants-2001_06 |
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| ORD ID | ord-ae249186fc9c49a49e13a037e1b1c221 |
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| Source note | uspto-grants-2001_06 |
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