참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | Formic Acid | HCID 284 | — |
| 반응물 | Hydrochloric Acid | HCID 313 | — |
| 반응물 | N-((1R,2R)-2-Amino-1,2-diphenylethyl)-4-methylbenzene-1-sulfonamide | HCID 2734565 | — |
| 반응물 | (R)-4-Acetyl-1-((S)-1-(4-methoxyphenyl)ethyl)pyrrolidin-2-one | HCID 58071853 | — |
| 촉매 | Bis[(pentamethylcyclopentadienyl)dichloro-rhodium] | HCID 16212157 | — |
| 용매 | Acetonitrile | HCID 6342 | — |
| 용매 | Triethylamine | HCID 8471 | — |
| 생성물 | (R)-4-((S)-1-hydroxyethyl)-1-((S)-1-(4-methoxyphenyl)ethyl)pyrrolidin-2-one | HCID 58071870 | — |
반응 단계
2.4 g of Dichloro-(pentamethylcyclopentadienyl)-rhodium-(III)-dimer and 2.8 g (R,R)—N-(p-toluenesulfonyl)-1,2-diphenylethylendiamine [(R,R)-TsDPEN] is added to a solution of 50 g (R)-4-acetyl-1-[(S)-1-(4-methoxyphenyl)-ethyl]-pyrrolidine-2-one in acetonitril at 25° C. The solution is cooled to −15° C. At this temperature a mixture of 22 mL formic acid and 135 mL triethylamine is added. The reaction mixture is stirred for 22 hours at −15° C. and then warmed up to 20° C. 230 mL of a 4 molar hydrochloric acid is added under cooling. The aqueous phase is extracted 3 times with ethyl acetate. The organic phase is washed with diluted and concentrated brine and treated with activated carbon. The organic phase is dried over sodium sulfate. The solvent is evaporated under reduced pressure to obtain
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 특허 번호 | US08912173B2 |
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| 출처 데이터셋 | uspto-grants-2014_12 |
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| ORD ID | ord-f1540f843dc5467eb5b5846804a77e85 |
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| 출처 메모 | uspto-grants-2014_12 |
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