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Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 70101생성일: 2026년 10월 23일

Water → (R)-2-{2-[4-(4-CHLORO-PHENYL)-PIPERAZIN-1-YL]-5-OXO-6,7-DIHYDRO-5H-5lambda4-THIENO-[3,2-D]PYRIMIDIN-4-YLAMINO}-3-METHYL-BUTAN-1-OL

https://huagongshe.com/ko/reaction/70101

반응식

참여 물질

역할이름HCID투입량
반응물WaterHCID 962—
반응물DiisopropylethylamineHCID 81531—
반응물D-ValinolHCID 6950587—
반응물4-Chloro-2-[4-(4-chloro-phenyl)-piperazin-1-yl]-6,7-dihydro-thieno[3,2-d]pyrimidine 5-oxideHCID 59475895—
용매1,4-DioxaneHCID 31275—
생성물(R)-2-{2-[4-(4-CHLORO-PHENYL)-PIPERAZIN-1-YL]-5-OXO-6,7-DIHYDRO-5H-5lambda4-THIENO-[3,2-D]PYRIMIDIN-4-YLAMINO}-3-METHYL-BUTAN-1-OLHCID 59475912—

반응 조건

온도120 °C

반응 단계

220 mg 4-chloro-2-[4-(4-chloro-phenyl)-piperazin-1-yl]-6,7-dihydro-thieno[3,2-d]pyrimidine 5-oxide (cf Example 124), 118.43 mg (R)-(−)-2-amino-3-methyl-butan-1-ol and 197.52 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 mixed with water, the precipitate formed is suction filtered, washed and dried. The diastereomers are separated by preparative HPLC (method B). 25.5 mg of Diastereomer 1 (Example 54) and 40.5 mg of Diastereomer 2 (Example 57) are obtained as a powder. Analytical HPLC (method A): Diastereomer I: RT=3.61 min; Diastereomer 2, RT=3.71 min.

출처 및 근거

DOI10.6084/m9.figshare.5104873.v1
특허 번호US08822474B2
출처 데이터셋uspto-grants-2014_09
ORD IDord-1e7cedad7cd441eabe301eec4eeae6c0
출처 메모uspto-grants-2014_09