HuagongsheHuagongshe Chemistry Print Report · For research reference only
Trifluoroacetic acid → HCID 66931544, compound
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Trifluoroacetic acid | HCID 6422 | — |
| Reactant | Diisopropylethylamine | HCID 81531 | — |
| Reactant | Methanaminium, N-((dimethylamino)(3H-1,2,3-triazolo(4,5-b)pyridin-3-yloxy)methylene)-N-methyl-, hexafluorophosphate(1-) (1:1) | HCID 9886157 | — |
| Reactant | 5-Chloro-3-fluoropyridine-2-carboxylic acid | HCID 11769070 | — |
| Reactant | HCID 66931535 | HCID 66931535 | — |
| Solvent | Dichloromethane | HCID 6344 | — |
| Product | HCID 66931544 | HCID 66931544 | 24% |
Reaction Steps
In analogy to example 22 a) the reaction of 5-chloro-3-fluoro-pyridine-2-carboxylic acid and Building block J, [(R)-5-(5-amino-2-fluoro-phenyl)-5-methyl-5,6-dihydro-2H-[1,4]oxazin-3-yl]-[bis-(4-methoxy-phenyl)-phenyl-methyl]-amine, using O-(7-azabenzotriazol-1-yl)-N,N,N′,N′-tetramethyluronium hexafluorophosphate as the condensating agent in presence of Huenig's base, followed by the cleavage of the [bis-(4-methoxy-phenyl)-phenyl-methyl]-(DMTr) amino protecting group with trifluoroacetic acid in dichloromethane yielded the title compound (yield: 24% of theory). Mass (calculated) C17H15ClF2N4O2.ClH [417.241]; (found) [M+H]+=381.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08188079B2 |
| Source dataset | uspto-grants-2012_05 |
| ORD ID | ord-012c391d86a6476197aa1b17e74357b2 |
| Source note | uspto-grants-2012_05 |