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HRID 885711作成日:2026年10月25日

Dicyclohexylcarbodiimide → (2R)-4-(4-oxo-4-(tetrahydro-2H-pyran-2-yloxyamino)butyl)phenyl 3-(5-(benzyloxy)pyridin-2-yl)-2-(tert-butoxycarbonylamino)propanoate

https://huagongshe.com/reaction/885711

反応式

関与物質

役割名称HCID仕込み量
反応物DicyclohexylcarbodiimideHCID 10868—
反応物(R)-3-(5-(Benzyloxy)pyridin-2-yl)-2-(tert-butoxycarbonylamino)propanoic acidHCID 67001556—
反応物4-(4-hydroxyphenyl)-N-(tetrahydro-2H-pyran-2-yloxy)butanamideHCID 86659508—
触媒4-(Dimethylamino)pyridineHCID 14284—
溶媒DichloromethaneHCID 6344—
生成物(2R)-4-(4-oxo-4-(tetrahydro-2H-pyran-2-yloxyamino)butyl)phenyl 3-(5-(benzyloxy)pyridin-2-yl)-2-(tert-butoxycarbonylamino)propanoateHCID 86659509—

反応条件

温度0 °C

反応手順

(R)-3-(5-(Benzyloxy)pyridin-2-yl)-2-(tert-butoxycarbonylamino)propanoic acid (0.19 g, 0.5 mmol), 4-(4-hydroxyphenyl)-N-(tetrahydro-2H-pyran-2-yloxy)-butanamide (0.14 g, 0.5 mmol), and DMAP (0.06 g, 0.5 mmol) were added into DCM (10 mL) and stirred at 0° C. for 10 min. A solution of DCC (0.12 g, 0.6 mmol) in DCM (5 mL) was added to the above-mentioned solution dropwise. The mixture was stirred from 0° C. at room temperature for 1 h (monitored by TLC). The white solid was removed and the filtrated was then evaporated in vacuo. Ethyl acetoacetate was added and the solid was again removed. The solution was evaporated in vacuo. The residue was purified by chromatography (EA:Hex=1:5) to give the title compound.

情報源と証拠

DOI10.6084/m9.figshare.5104873.v1
特許番号US08242282B2
出典データセットuspto-grants-2012_08
ORD IDord-7f74e26e32644d36818201dd646a826b
出典メモuspto-grants-2012_08