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4-Hydroxypyrrolidine → [(4S,5R)-2-(6-tert-Butyl-4-ethoxy-pyridin-3-yl)-4,5-bis-(4-chloro-phenyl)-4,5-dimethyl-4,5-dihydro-imidazol-1-yl]-[(1S,5R)-6-(3-hydroxy-pyrrolidine-1-carbonyl)-3-aza-bicyclo[3.1.0]hex-3-yl]-methanone
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | 4-Hydroxypyrrolidine | HCID 98210 | — |
| 反応物 | (1S,5R)-3-[(4S,5R)-2-(6-tert-butyl-4-ethoxy-pyridin-3-yl)-4,5-bis-(4-chloro-phenyl)-4,5-dimethyl-4,5-dihydro-imidazole-1-carbonyl]-3-aza-bicyclo[3.1.0]hexane-6-carboxylic acid | HCID 67204751 | — |
| 生成物 | [(4S,5R)-2-(6-tert-Butyl-4-ethoxy-pyridin-3-yl)-4,5-bis-(4-chloro-phenyl)-4,5-dimethyl-4,5-dihydro-imidazol-1-yl]-[(1S,5R)-6-(3-hydroxy-pyrrolidine-1-carbonyl)-3-aza-bicyclo[3.1.0]hex-3-yl]-methanone | HCID 57670049 | — |
反応手順
In a manner analogous to the method described in examples 99, (1S,5R)-3-[(4S,5R)-2-(6-tert-butyl-4-ethoxy-pyridin-3-yl)-4,5-bis-(4-chloro-phenyl)-4,5-dimethyl-4,5-dihydro-imidazole-1-carbonyl]-3-aza-bicyclo[3.1.0]hexane-6-carboxylic acid (prepared from the ethyl ester, example 135) was coupled with pyrrolidin-3-ol (Aldrich) to give the title compound as a mixture of diastereomers. HR-MS (ES, m/z) calculated for C39H46Cl2N5O4 [(M+H)+] 718.2922, observed 718.2921.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US08513239B2 |
| 出典データセット | uspto-grants-2013_08 |
| ORD ID | ord-1e0964ce55004567af05b247717f1ef2 |
| 出典メモ | uspto-grants-2013_08 |