Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Methanol | HCID 887 | — |
| Reactant | Methyl 2-[(2-chlorophenyl)methylidene]-3-oxobutanoate | HCID 299600 | — |
| Reactant | Ethyl 3-amino-4-(2-(1,3-dioxoisoindolin-2-yl)ethoxy)but-2-enoate | HCID 11174576 | — |
| Solvent | Isopropanol | HCID 3776 | — |
| Product | Phthalimidoamlodipine | HCID 9871958 | 69.6% |
Reaction Steps
Methyl 2-(2-chlorobenzyliden)acetoacetate (40.6 g; 169.9 mmol) was condensed with ethyl 3-amino-4-[2-(phthalimido)ethoxy]crotonate (51.5 g; 161.8 mmol) in 2-propanol (160 ml) under reflux for 11 hours. Methanol (103 ml) was added and mixture was cooled to 5/0° C. The solid was filtered off and dried at 40° C. Phthaloyl Amlodipine (60.7 g, purity: 98.6%; 0.86% of impurity HA) was obtained.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| Patent number | US07671208B2 |
|---|
| Source dataset | uspto-grants-2010_03 |
|---|
| ORD ID | ord-7c0a0754e20441159ba41fcc575d72d9 |
|---|
| Source note | uspto-grants-2010_03 |
|---|
