HuagongsheHuagongshe Chemistry Print Report · For research reference only
Piperidine → 4'-{(R)-1-[(3-Amino-oxetane-3-carbonyl)-amino]-ethyl}-3-chloro-3'-fluoro-biphenyl-2-carboxylic acid methyl ester
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Piperidine | HCID 8082 | — |
| Reactant | 3-Chloro-4'-((R)-1-{[3-(9H-fluoren-9-ylmethoxycarbonylamino)-oxetane-3-carbonyl]-amino}-ethyl)-3'-fluoro-biphenyl-2-carboxylic acid methyl ester | HCID 67979309 | — |
| Solvent | Dimethylformamide | HCID 6228 | — |
| Product | 4'-{(R)-1-[(3-Amino-oxetane-3-carbonyl)-amino]-ethyl}-3-chloro-3'-fluoro-biphenyl-2-carboxylic acid methyl ester | HCID 67979497 | — |
Reaction Steps
To a solution of 3-chloro-4′-((R)-1-{[3-(9H-fluoren-9-ylmethoxycarbonylamino)-oxetane-3-carbonyl]-amino}-ethyl)-3′-fluoro-biphenyl-2-carboxylic acid methyl ester (100 mg, 159 μmol, step C) in dry DMF (1.8 ml) was added piperidine (0.2 ml) and the solution was stirred at room temperature for 2 h. The brown solution was concentrated to dryness under high vacuum. The remaining residue was purified by chromatography (silica gel; DCM/MeOH 98:2) and the title compound was obtained as white solid (60 mg, 92%). MS: 407.2 [M+H]+.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08912221B2 |
| Source dataset | uspto-grants-2014_12 |
| ORD ID | ord-f1dc5266dbb94872b3898c60f04ea889 |
| Source note | uspto-grants-2014_12 |