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Ethyl 2-[(5-amino-1,3,4-thiadiazol-2-yl)sulfanyl]acetate → (2s,4s)-1-[[n-[4-[n-(5-Ethoxycarbonylmethylthio-1,3,4-thiadiazol-2-yl)amino]carbonylbicyclo[2.2.2]oct-1-yl]amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile
関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|---|---|---|
| 反応物 | Ethyl 2-[(5-amino-1,3,4-thiadiazol-2-yl)sulfanyl]acetate | HCID 351912 | — |
| 反応物 | (2S,4S)-1-[[N-(4-carboxybicyclo[2,2,2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile | HCID 57634365 | — |
| 生成物 | (2s,4s)-1-[[n-[4-[n-(5-Ethoxycarbonylmethylthio-1,3,4-thiadiazol-2-yl)amino]carbonylbicyclo[2.2.2]oct-1-yl]amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile | HCID 68843700 | 20.2% |
反応手順
In a similar manner to Example 87, (2S,4S)-1-[[N-(4-carboxybicyclo[2.2.2]oct-1-yl)amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile (50.0 mg) and ethyl[(5-amino-1,3,4-thiadiazol-2-yl)thio]acetate (74.6 mg) were used to obtain (2S,4S)-1-[[N-[4-[N-(5-ethoxycarbonylmethylthio-1,3,4-thiadiazol-2-yl)amino]carbonylbicyclo[2.2.2]oct-1-yl]amino]acetyl]-4-fluoropyrrolidine-2-carbonitrile (16.4 mg).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|---|
| 特許番号 | US07560569B2 |
| 出典データセット | uspto-grants-2009_07 |
| ORD ID | ord-4a6c2905117048fb8fb956b1775f2c17 |
| 出典メモ | uspto-grants-2009_07 |