Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 70097생성일: 2026년 10월 23일
Water → (3R,5S)-1-{2-[4-(4-chloro-phenyl)-piperazin-1-yl]-5-oxo-6,7-dihydro-5H-5lambda4-thieno[3,2-d]pyrimidin-4-yl}-5-hydroxymethyl-pyrrolidin-3-ol
https://huagongshe.com/ko/reaction/70097
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 | (3R,5S)-5-hydroxymethyl-pyrrolidin-3-ol trifluoroacetate | HCID 66735651 | — |
| 용매 | Dichloromethane | HCID 6344 | — |
| 용매 | 1,4-Dioxane | HCID 31275 | — |
| 생성물 | (3R,5S)-1-{2-[4-(4-chloro-phenyl)-piperazin-1-yl]-5-oxo-6,7-dihydro-5H-5lambda4-thieno[3,2-d]pyrimidin-4-yl}-5-hydroxymethyl-pyrrolidin-3-ol | HCID 59708409 | 75.7% |
반응 단계
220 mg (0.57 mmol) 4-chloro-2-[4-(4-chloro-phenyl)-piperazin-1-yl]-6,7-dihydro-thieno[3,2-d]pyrimidine 5-oxide, 159.23 mg (0.69 mmol) (3R,5S)-5-hydroxymethyl-pyrrolidin-3-ol trifluoroacetate (prepared from commercial Boc-trans-4-hydroxy-L-prolinol) and 197.52 μl (1.15 mmol) diisopropylethylamine are placed in 4 ml dioxane, and heated to 120° C. in the microwave for 0.3 hours. Then the reaction mixture is combined with water and dichloromethane and extracted. The organic phase is separated off using a phase separation cartridge and evaporated to dryness. 200.3 mg of the product (75%) are obtained as a racemic mixture. Analytical HPLC-MS (method A): RT=2.26 min.
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 특허 번호 | US08822474B2 |
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| 출처 데이터셋 | uspto-grants-2014_09 |
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| ORD ID | ord-ec8bf9e1cbfe48b789032d5231959db7 |
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| 출처 메모 | uspto-grants-2014_09 |
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