関与物質
| 役割 | 名称 | HCID | 仕込み量 |
|---|
| 反応物 | Triphenylphosphine | HCID 11776 | — |
| 反応物 | Diisopropyl azodicarboxylate | HCID 5363146 | — |
| 反応物 | Methyl 3-(benzyloxy)-5-hydroxybenzoate | HCID 7472028 | — |
| 反応物 | (2R)-1-{[Tri(propan-2-yl)silyl]oxy}propan-2-ol | HCID 57504697 | — |
| 溶媒 | Tetrahydrofuran | HCID 8028 | — |
| 生成物 | methyl 3-(benzyloxy)-5-{(1S)-1-methyl-2-[(triisopropylsilyl)oxy]ethoxy}benzoate | HCID 53629622 | 71.4% |
反応手順
(2R)-1-[(Triisopropylsilyl)oxy]propan-2-ol (56.1 g, 242 mmol) was added to a solution of methyl 3-hydroxy-5-{[phenylmethyl]oxy}benzoate (50 g, 194 mmol) and triphenylphosphine (63.5 g, 242 mmol) in dry THF (500 mL), at to 0° C., followed by addition of DIAD (47.6 mL, 242 mmol) over 45 minutes under an argon atmosphere. The reaction was stirred at 0° C. for 1 hour and allowed to warm up to RT over an hour then stirred at RT for 1 hour. The THF was evaporated and a mixture of ethyl acetate (80 mL) and hexane (120 mL) was added. This mixture stirred for 2 hours and filtered. The precipitate was washed with a mixture of ethyl acetate (20 mL) and hexane (180 mL) and the filtrate evaporated. The residue was purified by column chromatography, eluting with 1:20 to 1:10 ethyl acetate:hexanes, to afford the title compound (65.5 g).
情報源と証拠
| DOI | 10.6084/m9.figshare.5104873.v1 |
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| 特許番号 | US07977328B2 |
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| 出典データセット | uspto-grants-2011_07 |
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| ORD ID | ord-74e98af1b9cc40f49151d41863342dad |
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| 出典メモ | uspto-grants-2011_07 |
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