HuagongsheHuagongshe Chemistry Print Report · For research reference only
3-(Trifluoromethyl)azetidin-3-ol hydrochloride → [6-(Cyclopropylmethoxy)-5-(3,3-difluoroazetidin-1-yl)pyridin-2-yl]-[3-hydroxy-3-(trifluoromethyl)azetidin-1-yl]methanone
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 3-(Trifluoromethyl)azetidin-3-ol hydrochloride | HCID 46735152 | — |
| Reactant | 6-(Cyclopropylmethoxy)-5-(3,3-difluoroazetidin-1-yl)picolinic acid | HCID 71087292 | — |
| Product | [6-(Cyclopropylmethoxy)-5-(3,3-difluoroazetidin-1-yl)pyridin-2-yl]-[3-hydroxy-3-(trifluoromethyl)azetidin-1-yl]methanone | HCID 76281600 | 56% |
Reaction Steps
In analogy to the procedure described in Example 127 e), 6-cyclopropylmethoxy-5-(3,3-difluoro-azetidin-1-yl)-pyridine-2-carboxylic acid (Example 1 b, 40 mg, 141 μmol) was reacted with 3-(trifluoromethyl)azetidin-3-ol hydrochloride (CAN 848192-96-1, 30.0 mg, 169 μmol) to obtain the title compound (32 mg, 56%) as off-white solid, MS (EI): m/e=408.3 [MH+].
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US09303012B2 |
| Source dataset | uspto-grants-2016_04 |
| ORD ID | ord-98a49092a23c4b0d8c0f942c0a89617c |
| Source note | uspto-grants-2016_04 |