Water → [(R)-1-(6-chloro-1H-benzimidazol-2-yl)-2-methoxy-ethyl]-{2-[4-(4-chloro-phenyl)-piperazin-1-yl]-5-oxo-6,7-dihydro-5H-5lambda4-thieno[3,2-d]pyrimidin-4-yl}-amine

https://huagongshe.com/ko/reaction/70107

참여 물질

역할	이름	HCID	투입량
반응물	Water	HCID 962	—
반응물	Diisopropylethylamine	HCID 81531	—
반응물	4-Chloro-2-[4-(4-chloro-phenyl)-piperazin-1-yl]-6,7-dihydro-thieno[3,2-d]pyrimidine 5-oxide	HCID 59475895	—
반응물	(1R)-1-(5-chloro-1H-benzimidazol-2-yl)-2-methoxyethylamine	HCID 59708426	—
용매	Dichloromethane	HCID 6344	—
용매	1,4-Dioxane	HCID 31275	—
생성물	[(R)-1-(6-chloro-1H-benzimidazol-2-yl)-2-methoxy-ethyl]-{2-[4-(4-chloro-phenyl)-piperazin-1-yl]-5-oxo-6,7-dihydro-5H-5lambda4-thieno[3,2-d]pyrimidin-4-yl}-amine	HCID 59708429	37.8%

반응 조건

온도	120 °C

반응 단계

200 mg 4-chloro-2-[4-(4-chloro-phenyl)-piperazin-1-yl]-6,7-dihydro-thieno[3,2-d]pyrimidine 5-oxide (cf Example 124), 235 mg (R)-1-(6-chloro-1H-benzimidazol-2-yl)-2-methoxy-ethylamine and 179.62 μl diisopropylethylamine are placed in 4 ml dioxane, and the mixture is heated to 120° C. in the microwave for 0.3 hours. Then the reaction mixture is combined with water and dichloromethane and extracted. The product is purified by semipreparative HPLC (method A). 113 mg of the product are obtained as a powder. Analytical HPLC-MS, (method B): RT=1.88 min.

출처 및 근거

DOI	10.6084/m9.figshare.5104873.v1
특허 번호	US08822474B2
출처 데이터셋	uspto-grants-2014_09
ORD ID	ord-d01a71046514423f8d801eb4965992b8
출처 메모	uspto-grants-2014_09