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Sodium Chloride → 4-Nitrobenzyl 7-[2-(2-amino-4-thiazolyl)-2-ethoxyiminoacetamido]-3-cephem-4-carboxlate

HRID 434962
ノート
印刷プレビュー

反応式

HRID 434962 の反応式
P(Cl)(Cl)(Cl)=O.[NH2:6][C:7]1[S:8][CH:9]=[C:10]([C:12](=[N:16][O:17][CH2:18][CH3:19])[C:13]([OH:15])=O)[N:11]=1.C[Si](CC(N)=O)(C)C.[NH2:28][CH:29]1[C:49](=[O:50])[N:31]2[C:32]([C:36]([O:38][CH2:39][C:40]3[CH:45]=[CH:44][C:43]([N+:46]([O-:48])=[O:47])=[CH:42][CH:41]=3)=[O:37])=[CH:33][CH2:34][S:35][C@H:30]12.C(=O)(O)[O-].[Na+].[Cl-].[Na+]>O1CCCC1.O.CN(C)C=O>[NH2:6][C:7]1[S:8][CH:9]=[C:10]([C:12](=[N:16][O:17][CH2:18][CH3:19])[C:13]([NH:28][CH:29]2[C:49](=[O:50])[N:31]3[C:32]([C:36]([O:38][CH2:39][C:40]4[CH:41]=[CH:42][C:43]([N+:46]([O-:48])=[O:47])=[CH:44][CH:45]=4)=[O:37])=[CH:33][CH2:34][S:35][C@H:30]23)=[O:15])[N:11]=1
参加物実験手順後処理出典と根拠反応ノート

参加物

10

反応物 6

HCID 5234Sodium ChlorideHCID 24813Phosphorus oxychlorideHCID 357676Acetamide, 2-(trimethylsilyl)-2 回HCID 516892Sodium BicarbonateHCID 12775080p-Nitrobenzyl 7-amino-3-cephem-4-carboxylateHCID 534242352-(2-Amino-4-thiazolyl)-2-ethoxyiminoacetic acid

生成物 1

HCID 131712451
4-Nitrobenzyl 7-[2-(2-amino-4-thiazolyl)-2-ethoxyiminoacetamido]-3-cephem-4-carboxlate
収率 104.9%

試薬・触媒・溶媒 3

HCID 962Water溶媒HCID 6228Dimethylformamide溶媒HCID 8028Tetrahydrofuran溶媒3 回

実験手順

Phosphoryl chloride (1.764 g.) was added to a suspension of 2-(2-amino-4-thiazolyl)-2-ethoxyiminoacetic acid (syn isomer, 1.0 g.) in tetrahydrofuran (10 ml.) below 5° C. and stirred at the same temperature for 20 minutes. To the solution were added trimethylsilylacetamide (0.4 g.) and N,N-dimethylformamide (0.4 g.), and the solution was stirred below 5° C. for 40 minutes [Solution A]. On the other hand, trimethylsilylacetamide (3.5 g.) was added to a suspension of 4-nitrobenzyl 7-amino-3-cephem-4-carboxylate (1.5 g.) in tetrahydrofuran (15 ml.), and stirred at room temperature for 1.5 hours. To the solution was added all at once the above Solution A at -20° C., and the solution was stirred at -5° to 0° C. for an hour. Water (20 ml.) was added to the resultant solution at -20° C., and the solution was adjusted to pH 7.5 with an aqueous solution of sodium bicarbonate. Tetrahydrofuran (70 ml.) and a saturated aqueous solution of sodium chloride (50 ml.) were added to the solution, and the solution was shaken sufficiently. The aqueous layer was separated and extracted with tetrahydrofuran. The tetrahydrofuran layer and extract were combined and washed with a saturated aqueous solution of sodium chloride. The solution was dried over magnesium sulfate and concentrated under reduced pressure. The residue was triturated with diisopropyl ether to give 4-nitrobenzyl 7-[2-(2-amino-4-thiazolyl)-2-ethoxyiminoacetamido]-3-cephem-4-carboxylate (syn isomer, 2.5 g.).

後処理

  1. stirringstirred at room temperature for 1.5 hours
  2. stirringthe solution was stirred at -5° to 0° C. for an hour
  3. stirringthe solution was shaken sufficiently
  4. customThe aqueous layer was separated
  5. extractionextracted with tetrahydrofuran
  6. extractionThe tetrahydrofuran layer and extract
  7. washwashed with a saturated aqueous solution of sodium chloride
  8. dry with materialThe solution was dried over magnesium sulfate
  9. concentrationconcentrated under reduced pressure
  10. customThe residue was triturated with diisopropyl ether

出典と根拠

ORDレコード
ord-9593162501fc40b39ed140dc3ec97627
出典データセット
uspto-grants-1983_08
DOI
10.6084/m9.figshare.5104873.v1
特許番号
US04399133

反応ノート

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