HuagongsheHuagongshe Chemistry Print Report · For research reference only
Water → HCID 16115266, compound
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Water | HCID 962 | — |
| Reactant | Triethylamine | HCID 8471 | — |
| Reactant | PyBOP | HCID 2724699 | — |
| Reactant | HCID 68689596 | HCID 68689596 | — |
| Solvent | Dimethylformamide | HCID 6228 | — |
| Solvent | Ethyl Acetate | HCID 8857 | — |
| Product | HCID 16115266 | HCID 16115266 | 49.8% |
Reaction Steps
A stirring solution of 2-(1-aminomethyl-3-oxo-4-trifluoromethyl-1,3-dihydro-isoindol-2-yl)-propionic acid hydrochloride (185 mg, 0.55 mmol) and triethylamine (268 mg, 2.65 mmol) in dry DMF (10 mL) was added benzotriazol-1-yloxy-tris(pyrrolodinyl)-phosphonium hexafluorophosphate (354 mg, 0.68 mmol). The reaction was stirred for 4 h and then conc. in vacuo to a yellow oil. The oil was partioned between water and ethyl acetate. The organic layer was separated, dried over Na2SO4, and conc. in vacuo to a yellow solid. The solid was purified by radial chromatography (silica gel, EtOAc) to give 84 mg of the desired product as a white solid. MS (ESI) 285 (M+H).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US07244843B2 |
| Source dataset | uspto-grants-2007_07 |
| ORD ID | ord-4395330838a0485da5f99cfe045c380b |
| Source note | uspto-grants-2007_07 |