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3-Pyridinemethanamine → (R)-2-(3-(4-fluorobenzyl)-4-methyl-2-oxoimidazolidin-1-yl)-4-methyl-N-(thiazol-5-ylmethyl)thiazole-5-carboxamide
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 3-Pyridinemethanamine | HCID 31018 | — |
| 反応物 | 5-(Aminomethyl)-1,3-thiazole | HCID 5304077 | — |
| 反応物 | (R)-2-(3-(4-fluorobenzyl)-4-methyl-2-oxoimidazolidin-1-yl)-4-methylthiazole-5-carboxylic acid | HCID 57919880 | — |
| 反応物 | (S)-2-(3-(4-fluorobenzyl)-4-methyl-2-oxoimidazolidin-1-yl)-4-methylthiazole-5-carboxylic acid | HCID 57919976 | — |
| 生成物 | (R)-2-(3-(4-fluorobenzyl)-4-methyl-2-oxoimidazolidin-1-yl)-4-methyl-N-(thiazol-5-ylmethyl)thiazole-5-carboxamide | HCID 57919791 | — |
反応手順
Following the procedure as described in Example 2, making variations as required to replace pyridin-3-ylmethanamine with thiazol-5-ylmethanamine and replace (S)-2-(3-(4-fluorobenzyl)-4-methyl-2-oxoimidazolidin-1-yl)-4-methylthiazole-5-carboxylic acid with (R)-2-(3-(4-fluorobenzyl)-4-methyl-2-oxoimidazolidin-1-yl)-4-methylthiazole-5-carboxylic acid the title compound was obtained as a white solid: mp 66-69° C. (hexane); 1H NMR (300 MHz, DMSO-d6) δ 8.93 (s, 1H), 8.62 (t, J=5.7 Hz, 1H), 7.75 (s, 1H), 7.36-7.31 (m, 2H), 7.17-7.12 (m, 2H), 4.58-4.53 (m, 3H), 4.26 (d, J=15.6 Hz, 1H), 4.15 (t, J=9.6 Hz, 1H), 3.74-3.67 (m, 1H), 3.51 (dd, J=10.1, 6.8 Hz, 1H), 2.43 (s, 3H), 1.22 (d, J=6.1 Hz, 3H); MS (ES+) m/z 445.6 (M+1).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08049016B2 |
| 出典データセット | uspto-grants-2011_11 |
| ORD ID | ord-25c811628f2444dda94c81d386adb316 |
| 出典メモ | uspto-grants-2011_11 |