HuagongsheHuagongshe Chemistry Print Report · For research reference only
4-Methylmorpholine → 2'-Chloro-5'-(3-cyclohexyl-ureido)-biphenyl-4-carboxylic acid {4-[4-(propane-1-sulfonyl)-piperazin-1-ylmethyl]-phenyl}-amide
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-(Propylsulfonyl)piperazin-1-yl)methyl]aniline | HCID 28273548 | — |
| Reactant | 2'-Chloro-5'-(3-cyclohexyl-ureido)-biphenyl-4-carboxylic acid | HCID 67373328 | — |
| Solvent | Dimethylformamide | HCID 6228 | — |
| Product | 2'-Chloro-5'-(3-cyclohexyl-ureido)-biphenyl-4-carboxylic acid {4-[4-(propane-1-sulfonyl)-piperazin-1-ylmethyl]-phenyl}-amide | HCID 67370821 | 14.5% |
Reaction Steps
A mixture of 2′-Chloro-5′-(3-cyclohexyl-ureido)-biphenyl-4-carboxylic acid (150 mg), 4-(4-(propane-1-sulfonyl)-piperazin-1-ylmethyl)-phenylamine (236 mg) and HBTU (228 mg) in dry DMF (5 ml) containing N-methylmorpholine (0.13 ml) was stirred at room temp for 18 h. The mixture was then evaporated and the residue purified by chromatography. Gradient elution with 3%-20% 20DCM:8EtOH:1NH3 in DCM over 30 mins gave a white solid (38 mg)
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08008303B2 |
| Source dataset | uspto-grants-2011_08 |
| ORD ID | ord-05497c3b64724012a4d16acb90c24e61 |
| Source note | uspto-grants-2011_08 |