참여 물질
| 역할 | 이름 | HCID | 투입량 |
|---|
| 반응물 | 3,4-dihydro-2H-pyran | HCID 8080 | — |
| 반응물 | Benzenesulfonic acid, 4-methyl-, compd. with pyridine (1:1) | HCID 466102 | — |
| 반응물 | Sodium Acetate | HCID 517045 | — |
| 반응물 | HCID 178418287 | HCID 178418287 | — |
| 용매 | Dichloromethane | HCID 6344 | — |
| 생성물 | 8-(tetrahydro-pyran-2-yloxymethyl)-3,4-dihydro-2H-naphthalen-1-one | HCID 21986089 | 55% |
반응 단계
The diol (Intermediate H3) (2.42 g, 13.5 mmol) was dissolved in CH2Cl2 (75 mL) and reacted with dihydropyran (1.3 mL, 13.8 mmol) and pyridinium para-toluene sulfonate (PPTS) (350 mg, 1.36 mmol) at rt for 18 h. The mixture was concentrated onto SiO2 and purified by chromatography with 10% EtOAc:Hx. The tetrahydropyranyl (THP) protected alcohol (2.02 g, 7.70 mmol) was dissolved in CH2Cl2 (10 mL) and added to a mixture of pyridinium chlorochromate (PCC) (4.9 g, 22.2 mmol), sodium acetate (310 mg, 3.56 mmol) and celite (˜10 g) in CH2Cl2 (100 mL). The mixture was reacted at rt for 18 h and filtered through celite. The residue was purified by chromatography on SiO2 with 20 to 30% EtOAc:Hx to yield 8-(tetrahydro-pyran-2-yloxymethyl)-3,4-dihydro-2H-naphthalen-1-one (Intermediate H4) (˜55%).
출처 및 근거
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 특허 번호 | US08071635B2 |
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| 출처 데이터셋 | uspto-grants-2011_12 |
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| ORD ID | ord-26fb8de37c0347dca34d59785605ecf1 |
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| 출처 메모 | uspto-grants-2011_12 |
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