HuagongsheHuagongshe Chemistry Print Report · For research reference only
Diisopropylethylamine → 1-(2-Amino-6-{[2-({2-[1-(cyclopropylmethyl)piperidin-4-yl]-7-(2,4-dichlorophenyl)-[1,2,4]triazolo[1,5-c]pyrimidin-5-yl}amino)ethyl]amino}pyridin-3-yl)-2,2,2-trifluoroethanone
Participants
| Role | Name | HCID | Charge |
|---|---|---|---|
| Reactant | Diisopropylethylamine | HCID 81531 | — |
| Reactant | HCID 58305976 | HCID 58305976 | — |
| Reactant | 1-{2-Amino-6-[(2-aminoethyl)amino]pyridin-3-yl}-2,2,2-trifluoroethanone hydrochloride | HCID 67060322 | — |
| Solvent | Dimethyl Sulfoxide | HCID 679 | — |
| Product | 1-(2-Amino-6-{[2-({2-[1-(cyclopropylmethyl)piperidin-4-yl]-7-(2,4-dichlorophenyl)-[1,2,4]triazolo[1,5-c]pyrimidin-5-yl}amino)ethyl]amino}pyridin-3-yl)-2,2,2-trifluoroethanone | HCID 66911471 | — |
Reaction Conditions
| Temperature | 130 °C |
|---|
Reaction Steps
50 mg (0.10 mmol) of 5-chloro-2-[1-(cyclopropylmethyl)piperidin-4-yl]-7-(2,4-dichlorophenyl)-[1,2,4]triazolo[1,5-c]pyrimidine (Example 47A), 35 mg (0.12 mmol) of 1-{2-amino-6-[(2-aminoethyl)amino]pyridin-3-yl}-2,2,2-trifluoroethanone hydrochloride (Example 13A) and 0.110 ml (0.6 mmol) of N,N-diisopropylethylamine were initially charged in 1 ml of DMSO. The mixture was heated in the microwave at 130° C. for 30 min. This gave, after purification of the crude product by preparative HPLC (Method 11), 32 mg (48% of theory) of the product as a solid.
Provenance & Evidence
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| Patent number | US08436003B2 |
| Source dataset | uspto-grants-2013_05 |
| ORD ID | ord-96812c84203044e88619ffaa3c67323b |
| Source note | uspto-grants-2013_05 |