HuagongsheHuagongshe Chemistry Print Report · For research reference only
Cyclopropanecarbonyl chloride → Azd-7295
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Cyclopropanecarbonyl chloride | HCID 77637 | — |
| Reactant | Diisopropylethylamine | HCID 81531 | — |
| Reactant | 5'-Amino-2'-trifluoromethoxy-biphenyl-4-carboxylic acid {4-[4-(propane-1-sulfonyl)-piperazin-1-ylmethyl]-phenyl}-amide | HCID 59822368 | — |
| Solvent | Tetrahydrofuran | HCID 8028 | — |
| Product | Azd-7295 | HCID 57339445 | 32.2% |
Reaction Steps
A stirred solution of 5′-amino-2′-trifluoromethoxy-biphenyl-4-carboxylic acid {4-[4-(propane-1-sulfonyl)-piperazin-1-ylmethyl]-phenyl}-amide (50 mg) in dry THF (1 ml) was treated with N,N-diisopropylethylamine (60 μl) followed by cyclopropane carbonyl chloride (18 mg). After 16 h the mixture was evaporated and the residue purified by chromatography. Gradient elution with 0%-30% 20DCM:8EtOH:1NH3 in DCM over 35 mins gave the title compound as an off-white solid (18 mg).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08008303B2 |
| Source dataset | uspto-grants-2011_08 |
| ORD ID | ord-8500c374c40841a18b778d57153e9a29 |
| Source note | uspto-grants-2011_08 |