関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Triethylamine | HCID 8471 | — |
| 反応物 | Dicyclohexylcarbodiimide | HCID 10868 | — |
| 反応物 | Dota | HCID 121841 | — |
| 反応物 | (S)-tert-Butyl 5-amino-2-((tert-butoxycarbonyl)amino)pentanoate | HCID 7006667 | — |
| 溶媒 | Dichloromethane | HCID 6344 | — |
| 生成物 | L-(-)-Ornithine | HCID 6262 | — |
反応手順
DOTA (1,4,7,10-tetraazacyclododecan-1,4,7,10-tetraacetic acid) 0.5 mmol and 1.5 mmol of triethylamine were dissolved in 10 ml DCM. 0.6 mmol of DCC was dissolved in 5 ml DCM and added to the mixture. The reaction was carried out for 1 hour at room temperature. The white crystals that appeared in the mixture were filtered out. 0.5 mmol of solid BOC-Orn-OtBu was added to the reaction. The reaction was carried out for 20 hours at room temperature. The mixture was filtered and the DCM was evaporated. The product was washed several times with ethanol and air-dried. Cleavage of the protecting groups (BOC, OtBu) was carried out in 1 ml TFA+5% water for 3 hours. The acid was evaporated in a vacuum over a KOH pellet. The final product, L-Orn(DOTA), was washed several times with diethyl ether and dried. The product was dissolved in water and lyophilized.
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
|---|
| 特許番号 | US08993278B2 |
|---|
| 出典データセット | uspto-grants-2015_03 |
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| ORD ID | ord-b66c91595ae343a8a9e2a05535ce8b6b |
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| 出典メモ | uspto-grants-2015_03 |
|---|