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Ethyl 4-ethynylbenzoate → 4-[5-(4-Chloro-phenyl)-7-cyclopropyl-pyrazolo[1,5-a]pyrimidin-3-ylethynyl]-N-methyl-benzamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Ethyl 4-ethynylbenzoate | HCID 15540683 | — |
| 反応物 | 5-(4-Chloro-phenyl)-7-cyclopropyl-3-iodo-pyrazolo[1,5-a]pyrimidine | HCID 67000875 | — |
| 反応物 | NH3 THF MeOH | HCID 86608128 | — |
| 生成物 | 4-[5-(4-Chloro-phenyl)-7-cyclopropyl-pyrazolo[1,5-a]pyrimidin-3-ylethynyl]-N-methyl-benzamide | HCID 11852216 | — |
反応手順
The title compound was prepared by reacting 5-(4-chloro-phenyl)-7-cyclopropyl-3-iodo-pyrazolo[1,5-a]pyrimidine (example C.5 step 4) (792 mg, 2.0 mmol) and ethyl 4-ethynyl-benzoate (350 mg, 2.0 mmol) according to general procedure II, and subsequently, heating the suspension of the obtained product in 1 M NH3/THF-MeOH (1:1) to 60° C. for 75 h. Obtained as a yellow solid (6 mg, 14%). MS (ISP) 427.3 [(M+H)+]; mp 214-216° C.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08063048B2 |
| 出典データセット | uspto-grants-2011_11 |
| ORD ID | ord-5e7c95fa91e64bc2a97d6010072d6052 |
| 出典メモ | uspto-grants-2011_11 |