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Methyl 1-(naphthalen-1-ylsulfonyl)piperidine-4-carboxylate → 1-(1-(Naphthalen-1-ylsulfonyl)piperidin-4-yl)cyclopropanol

HRID 2356214
ノート
印刷プレビュー

反応式

HRID 2356214 の反応式
[CH2:1]([Mg]Br)[CH3:2].[C:5]1([S:15]([N:18]2[CH2:23][CH2:22][CH:21]([C:24](OC)=[O:25])[CH2:20][CH2:19]2)(=[O:17])=[O:16])[C:14]2[C:9](=[CH:10][CH:11]=[CH:12][CH:13]=2)[CH:8]=[CH:7][CH:6]=1>O1CCCC1.CC(C)[O-].CC(C)[O-].CC(C)[O-].C[Ti+3]>[C:5]1([S:15]([N:18]2[CH2:19][CH2:20][CH:21]([C:24]3([OH:25])[CH2:2][CH2:1]3)[CH2:22][CH2:23]2)(=[O:16])=[O:17])[C:14]2[C:9](=[CH:10][CH:11]=[CH:12][CH:13]=2)[CH:8]=[CH:7][CH:6]=1
参加物実験手順後処理出典と根拠反応ノート

参加物

5

反応物 2

HCID 11950392Methyl 1-(naphthalen-1-ylsulfonyl)piperidine-4-carboxylateHCID 178418443HCID 178418443、化合物

生成物 1

HCID 119503941-(1-(Naphthalen-1-ylsulfonyl)piperidin-4-yl)cyclopropanol収率 35.2%

試薬・触媒・溶媒 2

HCID 178459133HCID 178459133、化合物触媒HCID 8028Tetrahydrofuran溶媒

実験手順

Ethylmagnesium bromide (0.110 mL, 3.0 M in THF, 0.330 mmol) was added dropwise to a stirring solution of methyl 1-(naphthalen-1-ylsulfonyl)piperidine-4-carboxylate (0.100 g, 0.30 mmol) and methyltitanium triisopropoxide (0.300 mL, 1.0 M in THF, 0.300 mmol) in tetrahydrofuran (3 mL) at 0° C. The reaction mixture was allowed to warm to ambient temperature over 2 h then quenched with water (15 mL). The resulting flocculent solution was diluted with ethyl acetate (15 mL) and filtered through Celite. The filtrate was extracted with ethyl acetate (2×10 mL). The combined organic extracts were dried over anhydrous sodium sulfate and concentrated in vacuo. The resulting residue was purified by column chromatography on SiO2 eluted with hexanes/ethyl acetate (1:1) to yield 0.035 g (35%) of the title compound as a white foam. 1H NMR (400 MHz, Chloroform-d) δ, ppm: 0.36-0.41 (m, 2 H), 0.67-0.71 (m, 2H), 0.90-0.98 (m, 1 H), 1.72 (dd, J=13.89, 1.26 Hz, 2 H), 2.49 (td, J=12.51, 2.53 Hz, 2 H), 3.91-4.02 (m, 2 H), 7.54-7.60 (m, 3 H), 7.92 (d, J=8.34 Hz, 1 H), 8.06 (d, J=8.08 Hz, 1 H), 8.21 (d, J=7.33 Hz, 1 H), 8.76 (s, 1 H); ESI-MS: m/z 332.3 (M+H)+.

後処理

  1. customthen quenched with water (15 mL)
  2. additionThe resulting flocculent solution was diluted with ethyl acetate (15 mL)
  3. filtrationfiltered through Celite
  4. extractionThe filtrate was extracted with ethyl acetate (2×10 mL)
  5. dry with materialThe combined organic extracts were dried over anhydrous sodium sulfate
  6. concentrationconcentrated in vacuo
  7. customThe resulting residue was purified by column chromatography on SiO2
  8. washeluted with hexanes/ethyl acetate (1:1)

出典と根拠

ORDレコード
ord-255f06bbf0e749c5bb7ad73addb877d5
出典データセット
uspto-grants-2010_07
DOI
10.6084/m9.figshare.5104873.v1
特許番号
US07759339B2

反応ノート

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