HuagongsheHuagongshe Chemistry Print Report · For research reference only
3,3-Difluoroazetidine hydrochloride → 6-(3,3-Difluoro-azetidin-1-yl)-N-(3-iodo-4-methyl-phenyl)-nicotinamide
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 3,3-Difluoroazetidine hydrochloride | HCID 2758247 | — |
| Reactant | 6-chloro-N-(3-iodo-4-methyl-phenyl)-nicotinamide | HCID 7925562 | — |
| Reactant | N-(3-Iodo-4-methyl-phenyl)-6-morpholin-4-yl-nicotinamide | HCID 17541675 | — |
| Product | 6-(3,3-Difluoro-azetidin-1-yl)-N-(3-iodo-4-methyl-phenyl)-nicotinamide | HCID 59318130 | 40% |
Reaction Steps
6-(3,3-Difluoro-azetidin-1-yl)-N-(3-iodo-4-methyl-phenyl)-nicotinamide was prepared from 6-chloro-N-(3-iodo-4-methyl-phenyl)-nicotinamide and 3,3-difluoroazetidine hydrochloride in a manner similar to the one described in the synthesis of N-(3-Iodo-4-methyl-phenyl)-6-morpholin-4-yl-nicotinamide above. The product was isolated after silica gel column purification with 20-30% EtOAc in hexanes to afford the product (23 mg. Yield: 40%). HRMS m/z calcd for C16H14N3OFI [M+H]+: 430.0223. Found: 430.0224.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08324385B2 |
| Source dataset | uspto-grants-2012_12 |
| ORD ID | ord-a9b1db90ddcd465ab04c601fed358529 |
| Source note | uspto-grants-2012_12 |