HuagongsheHuagongshe Chemistry Print Report · For research reference only
4-Methylmorpholine → (S)-2-{4'-[4-(4-Methanesulfonyl-piperazin-1-ylmethyl)-phenylcarbamoyl]-6-trifluoromethoxy-biphenyl-3-ylcarbamoyl}-azetidine-1-carboxylic acid tert-butyl ester
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 4-Methylmorpholine | HCID 7972 | — |
| Reactant | Methanaminium, N-((1H-benzotriazol-1-yloxy)(dimethylamino)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1) | HCID 2733084 | — |
| Reactant | 4-(4-Methanesulfonyl-piperazin-1-ylmethyl)-phenylamine | HCID 11369231 | — |
| Reactant | (S)-2-(4'-Carboxy-6-trifluoromethoxy-biphenyl-3-ylcarbamoyl)-azetidine-1-carboxylic acid tert-butyl ester | HCID 67374213 | — |
| Solvent | Water | HCID 962 | — |
| Solvent | Dimethylformamide | HCID 6228 | — |
| Product | (S)-2-{4'-[4-(4-Methanesulfonyl-piperazin-1-ylmethyl)-phenylcarbamoyl]-6-trifluoromethoxy-biphenyl-3-ylcarbamoyl}-azetidine-1-carboxylic acid tert-butyl ester | HCID 67372397 | — |
Reaction Steps
A mixture of (S)-2-(4′-Carboxy-6-trifluoromethoxy-biphenyl-3-ylcarbamoyl)-azetidine-1-carboxylic acid tert-butyl ester (50 mg), 4-(4-methanesulfonyl-piperazin-1-ylmethyl)-phenylamine (29 mg), HBTU (61 mg) and N-methyl morpholine (0.033 ml) in dry DMF (3 ml) was stirred at room temp for 18 h. Water (10 ml) was then added and the cream solid collected by filtration and used without purification or characterisation.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08008303B2 |
| Source dataset | uspto-grants-2011_08 |
| ORD ID | ord-38e48f92abae4795bad99f7a41f92f08 |
| Source note | uspto-grants-2011_08 |