HuagongsheHuagongshe Chemistry Print Report · For research reference only
4,4-Difluoropiperidine hydrochloride → (4,4-Difluoro-piperidin-1-yl)-{5-[3-(4-fluoro-phenyl)-5-hydroxymethyl-isoxazol-4-ylmethoxy]-pyridin-2-yl}-methanone
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 4,4-Difluoropiperidine hydrochloride | HCID 2758351 | — |
| Reactant | 5-[3-(4-Fluoro-phenyl)-5-hydroxymethyl-isoxazol-4-ylmethoxy]-pyridine-2-carboxylic acid | HCID 66644394 | — |
| Product | (4,4-Difluoro-piperidin-1-yl)-{5-[3-(4-fluoro-phenyl)-5-hydroxymethyl-isoxazol-4-ylmethoxy]-pyridin-2-yl}-methanone | HCID 49804463 | 31% |
Reaction Steps
As described for example 34b, 5-[3-(4-fluoro-phenyl)-5-hydroxymethyl-isoxazol-4-ylmethoxy]-pyridine-2-carboxylic acid (75 mg, 0.22 mmol) was converted, using 4,4-difluoropiperidine hydrochloride instead of S-(+)-1-amino-2-propanol, to the title compound (45 mg, 31%), which was obtained as a colourless gum. MS: m/e=448.2 [M+H]+.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08415379B2 |
| Source dataset | uspto-grants-2013_04 |
| ORD ID | ord-134c7b5eb38140b7b7dd6f1f332361a8 |
| Source note | uspto-grants-2013_04 |