1,2-Diaminocyclohexane, trans- → 5-Chloro-N-((1-(4-(2-oxo-tetrahydropyrimidin-1(2H)-yl)phenyl)-1H-imidazol-4-yl)methyl)thiophene-2-carboxamide

참여 물질

역할	이름	HCID	투입량
반응물	1,2-Diaminocyclohexane, trans-	HCID 43806	—
반응물	Potassium Phosphate, Tribasic	HCID 62657	—
반응물	2(1H)-Pyrimidinone, tetrahydro-	HCID 74615	—
반응물	5-Chloro-N-((1-(4-iodophenyl)-1H-imidazol-4-yl)methyl)thiophene-2-carboxamide	HCID 24986897	—
촉매	Copper(1+) iodide; Copper(I) iodide; Cuprous iodide; Cuprous iodide (CuI)	HCID 24350	—
용매	1,4-Dioxane	HCID 31275	—
생성물	5-Chloro-N-((1-(4-(2-oxo-tetrahydropyrimidin-1(2H)-yl)phenyl)-1H-imidazol-4-yl)methyl)thiophene-2-carboxamide	HCID 24760093	5.3%

반응 조건

온도	110 °C

반응 단계

A mixture of 5-chloro-N-((1-(4-iodophenyl)-1H-imidazol-4-yl)methyl)thiophene-2-carboxamide 1-6 prepared in Example 1 (80 mg, 0.18 mmol), tetrahydro-2-pyrimidinone (54 mg, 0.54 mmol), 1,2-trans-diaminocyclohexane (13 μL, 0.11 mmol) and K3PO4 (100 mg, 0.47 mmol) in dioxane (1 mL) was degassed with Ar before being charged with CuI (20 mg, 0.11 mmol). The mixture in a sealed tube was heated at 110° C. overnight. It was then purified by HPLC to give the title compound (4 mg). MS 416.1 and 418.1 (M+H, Cl pattern).

출처 및 근거

DOI	10.6084/m9.figshare.5104873.v1
특허 번호	US08063077B2
출처 데이터셋	uspto-grants-2011_11
ORD ID	ord-48dc8b3e658e40d384deaa72515ab0ca
출처 메모	uspto-grants-2011_11