HuagongsheHuagongshe Chemistry Print Report · For research reference only
3-Methylazetidine hydrochloride → {3-(3-Cyclopropyl-1,2,4-oxadiazol-5-yl)-5-[4-(trifluoromethyl)phenyl]piperidin-1-yl}(3-methyl-azetidin-1-yl)methanone
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 3-Methylazetidine hydrochloride | HCID 25159188 | — |
| Reactant | 4-Nitrophenyl 3-(3-cyclopropyl-1,2,4-oxadiazol-5-yl)-5-[4-(trifluoromethyl)phenyl]piperidine-1-carboxylate | HCID 58002174 | — |
| Product | {3-(3-Cyclopropyl-1,2,4-oxadiazol-5-yl)-5-[4-(trifluoromethyl)phenyl]piperidin-1-yl}(3-methyl-azetidin-1-yl)methanone | HCID 58002596 | — |
Reaction Steps
95 mg (0.19 mmol) of the compound from Example 184A and 61 mg (0.57 mmol) of 3-methylazetidine hydrochloride were reacted according to the General Method 6. Work-up of the crude product was carried out initially by column chromatography on silica gel (mobile phase: dichloromethane->dichloromethane/methanol 100:5) and additionally by preparative HPLC. Yield: 14 mg (17% of theory)
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08119663B2 |
| Source dataset | uspto-grants-2012_02 |
| ORD ID | ord-a6dc42a042064022981a8d0e002db929 |
| Source note | uspto-grants-2012_02 |