HuagongsheHuagongshe Chemistry Print Report · For research reference only
4-Methylmorpholine → 5'-[2-(tert-Butoxycarbonyl-methyl-amino)-acetylamino]-2'-chloro-biphenyl-4-carboxylic acid ethyl ester
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 4-Methylmorpholine | HCID 7972 | — |
| Reactant | Glycine, N-[(1,1-dimethylethoxy)carbonyl]-N-methyl- | HCID 83692 | — |
| Reactant | Methanaminium, N-((1H-benzotriazol-1-yloxy)(dimethylamino)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1) | HCID 2733084 | — |
| Reactant | 5'-Amino-2'-chloro-biphenyl-4-carboxylic acid ethyl ester | HCID 59822374 | — |
| Solvent | Dimethylformamide | HCID 6228 | — |
| Product | 5'-[2-(tert-Butoxycarbonyl-methyl-amino)-acetylamino]-2'-chloro-biphenyl-4-carboxylic acid ethyl ester | HCID 67371228 | 40.6% |
Reaction Steps
A mixture of 5′-amino-2′-chloro-biphenyl-4-carboxylic acid ethyl ester (750 mg), (tert-butoxycarbonyl-methyl-amino)-acetic acid (589 mg) and HBTU (1.37 g) in dry DMF (40 ml) containing N-methylmorpholine (0.79 ml) was stirred at room temp for 18 h. The mixture was then evaporated and the residue was purified by chromatography. Elution with 4:1 petrol:ethyl acetate gave a pale brown oil (494 mg)
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08008303B2 |
| Source dataset | uspto-grants-2011_08 |
| ORD ID | ord-9d5fbf08eb4f49e7985984621f480f3d |
| Source note | uspto-grants-2011_08 |