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HRID 11851作成日:2026年10月27日

Diethylamine → (5-(N-Boc-N-2-picolylaminomethyl)pyrazine-2-carbonyl)-Ndelta-Cbz-L-ornithine

https://huagongshe.com/reaction/11851

反応式

関与物質

役割名称HCID仕込み量
反応物DiethylamineHCID 8021—
反応物1,3-Propanediamine, N'-(ethylcarbonimidoyl)-N,N-dimethyl-, monohydrochlorideHCID 2723939—
反応物H-Orn(Z)-OHHCID 7009570—
反応物5-(N-Boc-N-2-picolylaminomethyl)pyrazine-2-carboxylic AcidHCID 21973652—
触媒4-(Dimethylamino)pyridineHCID 14284—
溶媒DimethylformamideHCID 6228—
生成物(5-(N-Boc-N-2-picolylaminomethyl)pyrazine-2-carbonyl)-Ndelta-Cbz-L-ornithineHCID 86592263—

反応手順

The compound obtained in Example 8-6 (160 mg) was dissolved in DMF (3.2 ml) and diethylamine (0.32 ml) was added. After one hour, the reaction solution was concebtrated and the residue obtained was dissolved in DMF (1 ml). Then, WSCI hydrochloride (73 mg), DMAP (31 mg), and a solution of the compound obtained in Example 13-3 in DMF (1 ml) were sequentially added. After 15 hours, the reaction solution was concentrated. After the addition of chloroform and 1 mol/l hydrochloric acid, the residue was extracted with chloroform. The organic layer was washed with saturated brine and dried over anhydrous sodium sulfate. The residue was crude-purified by silica gel column chromatography (4 g, chloroform/ethyl acetate=1/2) to obtain the title compound (95.2 mg) as colorless syrup.

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-27b3171f15d74f3eb8897b1eb4d4be90
出典メモuspto-grants-2006_08