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HRID 11847作成日:2026年10月26日

1-Hydroxybenzotriazole → Nalpha-(2-(N-Boc-N-2-picolylaminomethyl)pyridin-5-ylcarbonyl)-Ndelta-Cbz-L-ornithine

https://huagongshe.com/reaction/11847

反応式

関与物質

役割名称HCID仕込み量
反応物1-HydroxybenzotriazoleHCID 75771—
反応物1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochlorideHCID 2723939—
反応物H-Orn(Z)-OHHCID 7009570—
反応物6-(N-Boc-N-2-picolylaminomethyl)nicotinic AcidHCID 21973663—
溶媒DimethylformamideHCID 6228—
生成物Nalpha-(2-(N-Boc-N-2-picolylaminomethyl)pyridin-5-ylcarbonyl)-Ndelta-Cbz-L-ornithineHCID 86592262107.6%

反応手順

The compound obtained in Example 8-6 (165.3 mg) was dissolved in DMF (3 ml). After the addition of WSCI hydrochloride (78.5 mg), HOBt (40.1 mg), and the compound obtained in Example 12-3 (90.4 mg), the mixture was stirred for 23 hours at room temperature. After the reaction, the solvent was removed by distillation. The residue was dissolved in chloroform and washed with 1 mol/l aqueous solution of hydrochloric acid, 1 mol/l aqueous solution of sodium hydroxide, and saturated brine. The organic layer was dried over anhydrous sodium sulfate and the solvent was removed by distillation. The residue was purified by silica gel column chromatography (10 g, chloroform/methanol=20/1) to obtain the title compound (167.6 mg) as white foam.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US07098215B2
出典データセットuspto-grants-2006_08
ORD IDord-5d6d23489ab9488382c98bbf6eb9445a
出典メモuspto-grants-2006_08