HuagongsheHuagongshe Chemistry Print Report · For research reference only
3,5-Difluoromandelic acid → 3-[N'-(3,5-Difluorophenyl-a-hydroxyacetyl)-L-alaninyl]amino-2,4-dioxo-1,5-bis-methyl-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 3,5-Difluoromandelic acid | HCID 588648 | — |
| Reactant | 3-(L-alaninyl)-amino-2,4-dioxo-1,5-bis-methyl-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine hydrochloride | HCID 69033234 | — |
| Product | 3-[N'-(3,5-Difluorophenyl-a-hydroxyacetyl)-L-alaninyl]amino-2,4-dioxo-1,5-bis-methyl-2,3,4,5-tetrahydro-1H-1,5-benzodiazepine | HCID 22984128 | — |
Reaction Steps
Following General Procedure I above using 3,5-difluoromandelic acid (Lancaster) and the product from Example 8-R, the title compound was prepared as an amorphous white solid. Purification was by L.C. 2000 eluting with straight EtOAc then flash chromatography eluting with CH2Cl2/Acetone (4:1 gradient to 3:1). Rf=0.39 and 0.34 (EtOAc).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US06667305B1 |
| Source dataset | uspto-grants-2003_12 |
| ORD ID | ord-24f76d61bacf4431aee15678a0273fdc |
| Source note | uspto-grants-2003_12 |