HuagongsheHuagongshe Chemistry Print Report · For research reference only
Water → {4'-[4-(4-Dimethylsulfamoyl-piperazin-1-ylmethyl)-phenylcarbamoyl]-6-trifluoromethoxy-biphenyl-3-yl}-carboxylic acid tert-butyl ester
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Water | HCID 962 | — |
| Reactant | 4-Methylmorpholine | HCID 7972 | — |
| Reactant | 1-Ethyl-3-(3'-dimethylaminopropyl)carbodiimide | HCID 15908 | — |
| Reactant | 1-Hydroxybenzotriazole | HCID 75771 | — |
| Reactant | 4-(4-Amino-benzyl)-piperazine-1-sulfonic acid dimethylamide | HCID 28273552 | — |
| Reactant | 5'-tert-Butoxycarbonylamino-2'-trifluoromethoxy-biphenyl-4-carboxylic acid | HCID 59822341 | — |
| Solvent | Dimethylformamide | HCID 6228 | — |
| Product | {4'-[4-(4-Dimethylsulfamoyl-piperazin-1-ylmethyl)-phenylcarbamoyl]-6-trifluoromethoxy-biphenyl-3-yl}-carboxylic acid tert-butyl ester | HCID 67373671 | — |
Reaction Steps
A mixture of 5′-tert-butoxycarbonylamino-2′-trifluoromethoxy-biphenyl-4-carboxylic acid (300 mg), 4-(4-amino-benzyl)-piperazine-1-sulfonic acid dimethylamide (226 mg), EDAC (144 mg) and HOBT (103 mg) in dry DMF (3 ml) containing N-methyl morpholine (0.166 ml) was stirred for 16 h. The mixture was then added to water (12 ml) and the resulting solid collected by filtration and dried and used in the following step without purification (558 mg)
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08008303B2 |
| Source dataset | uspto-grants-2011_08 |
| ORD ID | ord-ea056892380d44d4bf87895aaf8d113c |
| Source note | uspto-grants-2011_08 |