Huagongshe화공사 화학 정보 인쇄 보고서 · 연구 참고용
HRID 80623생성일: 2026년 10월 25일
3-Iodotoluene → (8S)-9-(3-methylphenyl)-2-(morpholin-4-yl)-8-(trifluoro-methyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one
https://huagongshe.com/reaction/80623
참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | 3-Iodotoluene | HCID 12268 | — |
| 반응물 | Potassium Phosphate, Tribasic | HCID 62657 | — |
| 반응물 | 1,2-Diaminocyclohexane, (+)- | HCID 479307 | — |
| 반응물 | (S)-8-(Morpholin-4-yl)-2-(trifluoromethyl)-1,2,3,4-tetrahydropyrimido[1,2-a]pyrimidin-6-one | HCID 136238743 | — |
| 촉매 | Copper iodide | HCID 83717 | — |
| 용매 | Dimethylformamide | HCID 6228 | — |
| 용매 | Dichloromethane | HCID 6344 | — |
| 용매 | Dichloromethane methanol | HCID 21226129 | — |
| 생성물 | (8S)-9-(3-methylphenyl)-2-(morpholin-4-yl)-8-(trifluoro-methyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]pyrimidin-4-one | HCID 49854400 | — |
반응 단계
The product is prepared according to the procedure described in Example 12, but using 250 mg of (8S)-2-morpholin-4-yl-8-trifluoromethyl-6,7,8,9-tetrahydropyrimido[1,2-a]pyrimidin-4-one (Example 1e) in 4 ml of dimethylformamide, 251 mg of 1-iodo-3-methylbenzene, 349 mg of tripotassium phosphate, 156 mg of copper iodide and 93 mg of (1S,2S)-cyclo-hexane-1,2-diamine. After 1 hour at 150° C. under microwave irradiation and silica column purification of the resulting reaction mixture (elution gradient of CH2Cl2 to CH2Cl2/MeOH 98/02), 195 mg of (88)-9-(3-methylphenyl)-2-(morpholin-4-yl)-8-(trifluoromethyl)-6,7,8,9-tetrahydro-4H-pyrimido[1,2-a]-pyrimidin-4-one are obtained in the form of a green solid, the characteristics of which are the following:
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 특허 번호 | US08846670B2 |
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| 출처 데이터셋 | uspto-grants-2014_09 |
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| ORD ID | ord-072e0694c5ce44418a2b16a7001210a6 |
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| 출처 메모 | uspto-grants-2014_09 |
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