Participants
| Role | Name | HCID | Charge |
|---|
| Reactant | Sodium Carbonate | HCID 10340 | — |
| Reactant | N-((4-bromo-1-trityl-1H-imidazol-2-yl)(5-ethoxy-2-fluoro-3-isopropoxyphenyl)methyl)-4-(5-methyl-1,2,4-oxadiazol-3-yl)benzenamine | HCID 68813809 | — |
| Solvent | Water 1,2-dimethoxyethane | HCID 18180031 | — |
| Product | HCID 68813792 | HCID 68813792 | — |
Reaction Steps
A suspension of 66.3 (100 mg, 0.13 mmol), 2-carboxyl phenylboronic acid (30 mg, 0.2 mmol), Na2CO3 (56 mg, 0.52 mmol) in 3:1 DME/H2O (3 mL) was degassed and then added in Pd(PPh3)4 (10 mg). The reaction mixture was heated to 170° C. for 15 mins in microwave. The reaction mixture was adjust to PH ˜4-5, then partitioned between EtOAc and sat. NaCl, the organic layer was collected and dried over (Na2SO4), filtered and concentrated to afford Intermediate 133.1. The crude material was used in the next step without further purification. LCMS (2 min grad.) RT=2.13 min, 814.3 (M+H).
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| Patent number | US07576098B2 |
|---|
| Source dataset | uspto-grants-2009_08 |
|---|
| ORD ID | ord-1322832f2f1a4b219026f3db6876d300 |
|---|
| Source note | uspto-grants-2009_08 |
|---|
