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1-Hydroxybenzotriazole → tert-Butyl trans(+/-)-3-{[(benzyloxy)carbonyl]amino}-4-{[(4-chloro-5-ethyl-1H-imidazol-2-yl)carbonyl]amino}piperidine-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 | 4-chloro-5-ethyl-1H-imidazole-2-carboxylic acid | HCID 67548929 | — |
| 反応物 | tert-Butyl trans(+/-)-4-amino-3-{[(benzyloxy)carbonyl]amino}piperidine-1-carboxylate | HCID 86648550 | — |
| 生成物 | tert-Butyl trans(+/-)-3-{[(benzyloxy)carbonyl]amino}-4-{[(4-chloro-5-ethyl-1H-imidazol-2-yl)carbonyl]amino}piperidine-1-carboxylate | HCID 86648552 | 69% |
反応手順
The same operation as in Example (1g) was performed using tert-butyl trans(±)-4-amino-3-{[(benzyloxy)carbonyl]amino}piperidine-1-carboxylate obtained in Example (79c) (98 mg, 0.28 mmol), 4-chloro-5-ethyl-1H-imidazole-2-carboxylic acid obtained by the method described in Example (1d) (48 mg, 0.25 mmol), WSC hydrochloride (150 mg, 0.78 mmol) and HOBT (35 mg, 0.26 mmol), to obtain 88.2 mg of the title compound as a white solid (69%).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08927588B2 |
| 出典データセット | uspto-grants-2015_01 |
| ORD ID | ord-5beae8d117c4487891783d40d5653af9 |
| 出典メモ | uspto-grants-2015_01 |