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N-(2-(p-bromophenoxy)ethyl)pyrrolidine → [8-(4-Methanesulfonyl-phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl]-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amine
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | N-(2-(p-bromophenoxy)ethyl)pyrrolidine | HCID 70657 | — |
| 反応物 | 8-(4-Methanesulfonyl-phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-ylamine | HCID 57502376 | — |
| 生成物 | [8-(4-Methanesulfonyl-phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl]-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amine | HCID 67479243 | — |
反応手順
[8-(4-Methanesulfonyl-phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-yl]-[4-(2-pyrrolidin-1-yl-ethoxy)-phenyl]-amine was prepared from 8-(4-methanesulfonyl-phenyl)-[1,2,4]triazolo[1,5-a]pyridin-2-ylamine (100.0 mg, 0.3468 mmol) and 1-[2-(4-bromo-phenoxy)-ethyl]-pyrrolidine (0.10 mL, 0.48 mmol) in a manner analogous to Step 2d. The title compound was isolated as a yellow solid (0.025 g, 15%). MP=170-173° C. 1H NMR (400 MHz, CDCl3, δ, ppm): 8.49-8.45 (m, 1H), 8.25-8.20 (m, 2H), 8.10-8.06 (m, 2H), 7.65-7.61 (m, 1H), 7.51-7.46 (m, 2H), 7.00 (t, J=6.9 Hz, 1H), 6.97-6.93 (m, 2H), 6.70 (s, 1H), 4.11 (t, J=6.1 Hz, 2H), 3.10 (s, 3H), 2.91 (t, J=6.0 Hz, 2H), 2.67-2.60 (m, 4H), 1.86-1.87 (m, 4H). MS=478 (MH)+.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08633173B2 |
| 出典データセット | uspto-grants-2014_01 |
| ORD ID | ord-4e78ae6fc4fa458188201077b0b686e0 |
| 出典メモ | uspto-grants-2014_01 |