HuagongsheHuagongshe Chemistry Print Report · For research reference only
Acetonitrile → 5-HT6/7 antagonist 1
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Acetonitrile | HCID 6342 | — |
| Reactant | Potassium Carbonate | HCID 11430 | — |
| Reactant | 3-(4-Piperidyl)-6-fluoro-1,2-benzisoxazole | HCID 849421 | — |
| Reactant | 2-Bromoethylphthalimide | HCID 21960021 | — |
| Product | 5-HT6/7 antagonist 1 | HCID 9865357 | — |
Reaction Steps
A mixture of 6-fluoro-3-(4-piperidinyl)-1,2-benzisoxazole (5.15 g, 23.4 mmol), K2CO3 (4.2 g, 30.4 mmol) and 2-bromoethyl phthalimide (7.13 g, 28 mmol) in acetonitrile (250 ml) was heated at reflux for 3.5 hours. The solids and solvent were removed. The residue was purified by flash chromatography (SiO2, 110 g, eluted with 2-4% CH3OH:DCM). The product thus obtained weighed 7.8 g (84%). Part of the material was recrystallized to give 2.35 g of off white crystals, m.p.=148°-149° C.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US05580887 |
| Source dataset | uspto-grants-1996_12 |
| ORD ID | ord-c22c8f796b02462ab96d7a677b6b3a7a |
| Source note | uspto-grants-1996_12 |