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(R)-2-Methyl-CBS-oxazaborolidine → (S)-ethyl 2-(2-bromo-5-methyl-7-(trifluoromethylsulfonyloxy)benzo[d]thiazol-6-yl)-2-hydroxyacetate

HRID 879260
ノート
印刷プレビュー

反応式

HRID 879260 の反応式
[Br:1][C:2]1[S:3][C:4]2[C:10]([O:11][S:12]([C:15]([F:18])([F:17])[F:16])(=[O:14])=[O:13])=[C:9]([C:19](=[O:25])[C:20]([O:22][CH2:23][CH3:24])=[O:21])[C:8]([CH3:26])=[CH:7][C:5]=2[N:6]=1.B1(C)OC(C2C=CC=CC=2)(C2C=CC=CC=2)[C@@H]2N1CCC2>C1(C)C=CC=CC=1>[Br:1][C:2]1[S:3][C:4]2[C:10]([O:11][S:12]([C:15]([F:18])([F:16])[F:17])(=[O:14])=[O:13])=[C:9]([C@H:19]([OH:25])[C:20]([O:22][CH2:23][CH3:24])=[O:21])[C:8]([CH3:26])=[CH:7][C:5]=2[N:6]=1
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

4

反応物 2

HCID 9838490(R)-2-Methyl-CBS-oxazaborolidineHCID 86699782Ethyl 2-(2-bromo-5-methyl-7-(trifluoromethylsulfonyloxy)benzo[d]thiazol-6-yl)-2-oxoacetate

生成物 1

HCID 86699783(S)-ethyl 2-(2-bromo-5-methyl-7-(trifluoromethylsulfonyloxy)benzo[d]thiazol-6-yl)-2-hydroxyacetate

試薬・触媒・溶媒 1

HCID 1140Toluene溶媒

反応条件

温度
-35 °C

実験手順

To a solution of 30 (8.30 g, 17.4 mmol) in toluene (70 mL) was added ((R)-2-methyl-CBS-oxazaborolidine (725 mg, 2.61 mmol). The reaction mixture was then cooled to −35° C. and a solution of catecholborane (freshly distilled) (1 M in toluene, 20.9 mL, 20.9 mmol) was added via addition funnel over 30 min. The reaction was stirred for 20 min while warming to −20° C. A 2 M solution of Na2CO3 was added (50 mL). The layers were separated, and the organic layer was washed with additional Na2CO3 solution (3×25 mL). The organic layer was dried, filtered, and concentrated in vacuo to give 31, which had analytical data to match 29. The compound was taken on to the next step without further purification.

後処理

  1. distillationa solution of catecholborane (freshly distilled) (1 M in toluene, 20.9 mL, 20.9 mmol)
  2. additionwas added via addition funnel over 30 min
  3. temperaturewhile warming to −20° C
  4. additionA 2 M solution of Na2CO3 was added (50 mL)
  5. customThe layers were separated
  6. washthe organic layer was washed with additional Na2CO3 solution (3×25 mL)
  7. customThe organic layer was dried
  8. filtrationfiltered
  9. concentrationconcentrated in vacuo

出典と根拠

ORDレコード
ord-6ed3ac39bdf2428fbd8f4a9a43b4e04e
出典データセット
uspto-grants-2015_03
DOI
10.6084/m9.figshare.5104873.v1
特許番号
US08987250B2

反応ノート

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