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Tetrahydrofuran → N-(3-Methylbutyl)-5-t-butyloxycarbonylamino 6-cyclohexyl-1-hexen-4-ol-2-carboxamide

HRID 345910
ノート
印刷プレビュー

反応式

HRID 345910 の反応式
[CH3:1][CH:2]([CH3:11])[CH2:3][CH2:4][NH:5][C:6](=[O:10])[C:7]([CH3:9])=[CH2:8].[CH2:12]([Li])[CH2:13][CH2:14][CH3:15].[C:17]([O:21][C:22]([N:24](C1CCCCC1)[C@H](C=O)C)=[O:23])([CH3:20])([CH3:19])[CH3:18].C(Cl)(Cl)Cl.[C:39](OCC)(=O)C.[O:45]1[CH2:49][CH2:48][CH2:47][CH2:46]1>CCCCCC.CC(C)[O-].CC(C)[O-].CC(C)[O-].Cl[Ti+3]>[CH3:1][CH:2]([CH3:11])[CH2:3][CH2:4][NH:5][C:6]([C:7]([CH2:9][CH:49]([OH:45])[CH:48]([NH:24][C:22]([O:21][C:17]([CH3:20])([CH3:19])[CH3:18])=[O:23])[CH2:47][CH:46]1[CH2:39][CH2:12][CH2:13][CH2:14][CH2:15]1)=[CH2:8])=[O:10]
参加物反応条件実験手順後処理出典と根拠反応ノート

参加物

8

反応物 5

HCID 8028Tetrahydrofuran2 回HCID 13877721Methacrylamide, N-(3-methylbutyl)-HCID 18606792Boc cyclohexylalaninalHCID 21584013Chloroform ethylacetateHCID 178418339Butyllithium

生成物 1

HCID 13877724N-(3-Methylbutyl)-5-t-butyloxycarbonylamino 6-cyclohexyl-1-hexen-4-ol-2-carboxamide

試薬・触媒・溶媒 2

HCID 11673339Chlorotitaniumtriisopropoxide触媒HCID 8058Hexane溶媒2 回

反応条件

温度
0 °C

実験手順

A solution of N-(3-methylbutyl)-2-methylpropenamide (643 mg, 4.15 mmol) in 25 ml of dry tetrahydrofuran was cooled under an N2 atmosphere to -78° C. and treated dropwise with 3.28 ml (8.5 mmol) of n-butyl-lithium in hexane. The resulting solution was warmed to 0° C. for 20 minutes, recooled to -78° C. and treated with 6.2 mL (6.2 mmol) of chlorotitanium triisopropoxide in hexane. After again warming to 0° C. for 5 minutes, the dark solution was recooled to -78° C. treated with a solution of N-t-butyloxycarbonyl-cyclohexylalaninal (670 mg, 2.3 mmol) in 5 ml of tetrahydrofuran, stirred for 5 minutes at -78° C., warmed to 0° C. for 20 minutes and quenched with saturated aqueous ammonium chloride. The resulting suspension was treated with ca. 50 ml of ether, stirred until the salts became white, extracted with two 100 ml portions of ether, dried over MgSO4 and concentrated in vacuo. The crude mixture was separated by flash column chromatography using 4:1 chloroform/ethyl acetate to give 249 mg (25%) of the (4S,5S) product (Rf 0.44), 292 mg (31%) of the (4R,5S) product (Rf 0.36, 3:2 chloroform/ethyl acetate) and 184 mg (20%) of a ca. 1:1 mixture of the two products. Mass spectrum: M+ =410.

後処理

  1. customrecooled to -78° C.
  2. temperatureAfter again warming to 0° C. for 5 minutes
  3. customwas recooled to -78° C.
  4. temperaturewarmed to 0° C. for 20 minutes
  5. customquenched with saturated aqueous ammonium chloride
  6. additionThe resulting suspension was treated with ca. 50 ml of ether
  7. stirringstirred until the salts
  8. extractionextracted with two 100 ml portions of ether
  9. dry with materialdried over MgSO4
  10. concentrationconcentrated in vacuo
  11. customThe crude mixture was separated by flash column chromatography
  12. customto give

出典と根拠

ORDレコード
ord-bfd223ee5835412e995e51a4c13a18de
出典データセット
uspto-grants-1991_10
DOI
10.6084/m9.figshare.5104873.v1
特許番号
US05059589

反応ノート

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