HuagongsheHuagongshe Chemistry Print Report · For research reference only
Ammonia → N-[4-(aminomethyl)phenyl]-alpha(R)-hydroxy-3-oxo-4-[4-(trifluoromethyl)phenyl]-2(R)-morpholineacetamide
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Ammonia | HCID 222 | — |
| Reactant | (R)-2-acetoxy-2-((R)-3-oxo-4-(4-(trifluoromethyl)phenyl)morpholin-2-yl)acetic acid | HCID 58181429 | — |
| Reactant | HCID 178418361 | HCID 178418361 | — |
| Catalyst | Nickel | HCID 935 | — |
| Solvent | Methanol | HCID 887 | — |
| Product | N-[4-(aminomethyl)phenyl]-alpha(R)-hydroxy-3-oxo-4-[4-(trifluoromethyl)phenyl]-2(R)-morpholineacetamide | HCID 58181437 | — |
Reaction Steps
To Compound 99-1 in 15 mL of 7M NH3 in MeOH was added excess Raney Ni (an aq. suspension) and the mixture stirred under a balloon of hydrogen for two hours. The mixture was filtered and evaporated to dryness yielding a white solid. Purification by RP-HPLC yielded 34 mg of EXAMPLE 99 as a white solid after conversion to the HCl salt by the addition of 1N HCl in diethyl ether and evaporation to dryness.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08642582B2 |
| Source dataset | uspto-grants-2014_02 |
| ORD ID | ord-edc2a7be543349599d6f8e00413e0824 |
| Source note | uspto-grants-2014_02 |