HuagongsheHuagongshe Chemistry Print Report · For research reference only
5-(Difluoromethoxy)picolinic acid → 5-Difluoromethoxy-pyridine-2-carboxylic acid [3-((R)-5-amino-3-methyl-1,1-dioxo-1,2,3,6-tetrahydro-1lambda6-[1,4]thiazin-3-yl)-4-fluoro-phenyl]-amide
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | 5-(Difluoromethoxy)picolinic acid | HCID 57475871 | — |
| Reactant | (R)-5-(5-amino-2-fluoro-phenyl)-5-methyl-1,1-dioxo-1,2,5,6-tetrahydro-1lambda6-[1,4]thiazin-3-ylamine | HCID 90067101 | — |
| Product | 5-Difluoromethoxy-pyridine-2-carboxylic acid [3-((R)-5-amino-3-methyl-1,1-dioxo-1,2,3,6-tetrahydro-1lambda6-[1,4]thiazin-3-yl)-4-fluoro-phenyl]-amide | HCID 72547962 | 52.1% |
Reaction Steps
Prepared from 5-(difluoromethoxy)picolinic acid (69.7 mg, 369 μmol, Eq: 1.00) and (R)-5-(5-amino-2-fluoro-phenyl)-5-methyl-1,1-dioxo-1,2,5,6-tetrahydro-1λ6-[1,4]thiazin-3-ylamine (100 mg, 369 μmol, Eq: 1.00) as described for example 2 (method b) to give the title compound (85 mg, 192 μmol, 52.1% yield) as a white foam. MS (ISP): m/z=443.4 [(M+H)].
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US09273042B2 |
| Source dataset | uspto-grants-2016_03 |
| ORD ID | ord-2153c01f58e246c4a7b4d292984b9700 |
| Source note | uspto-grants-2016_03 |