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1-Hydroxybenzotriazole → tert-Butyl cis(+/-)-4-{[(4,5-diiodo-1H-imidazol-2-yl)carbonyl]amino}-3-methoxypiperidine-1-carboxylate
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 1-Hydroxybenzotriazole | HCID 75771 | — |
| 反応物 | 1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochloride | HCID 2723939 | — |
| 反応物 | (3R,4S)-4-Amino-1-boc-3-methoxypiperidine | HCID 57362389 | — |
| 反応物 | 4,5-diiodo-1H-imidazole-2-carboxylic acid | HCID 67548481 | — |
| 生成物 | tert-Butyl cis(+/-)-4-{[(4,5-diiodo-1H-imidazol-2-yl)carbonyl]amino}-3-methoxypiperidine-1-carboxylate | HCID 86648535 | 43% |
反応手順
The same operation as in Example (1g) was performed using tert-butyl cis(±)-4-amino-3-methoxypiperidine-1-carboxylate obtained by the method described in Example (1e) (170 mg, 0.74 mmol), 4,5-diiodoimidazole-2-carboxylic acid obtained in Example (71b) (about 0.34 mmol), WSC hydrochloride (195 mg, 1.02 mmol) and HOBT (46 mg, 0.34 mmol), to obtain 83.1 mg of the title compound as a white solid (43%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08536197B2 |
| 出典データセット | uspto-grants-2013_09 |
| ORD ID | ord-15291c41996e4a0b8f04a1fc845dce6e |
| 出典メモ | uspto-grants-2013_09 |