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Phosphorus oxychloride → p-Nitrobenzyl 7-{2-(1,2,3-thiadiazol-4-yl)-2-methoxyiminoacetamido}-3-cephem-4-carboxylate

HRID 364527
ノート
印刷プレビュー

反応式

HRID 364527 の反応式
P(Cl)(Cl)([Cl:3])=O.[S:6]1[CH:10]=[C:9]([C:11](=[N:15][O:16][CH3:17])[C:12]([OH:14])=O)[N:8]=[N:7]1.[NH2:18][CH:19]1[C:39](=[O:40])[N:21]2[C:22]([C:26]([O:28][CH2:29][C:30]3[CH:35]=[CH:34][C:33]([N+:36]([O-:38])=[O:37])=[CH:32][CH:31]=3)=[O:27])=[CH:23][CH2:24][S:25][C@H:20]12.C[Si](CC(N)=O)(C)C.C[Si](C([Si](C)(C)C)C(N)=O)(C)C>C(OCC)(=O)C.O.CN(C)C=O>[CH3:20][N+:21]([CH3:39])=[CH:22][Cl:3].[Cl-:3].[S:6]1[CH:10]=[C:9]([C:11](=[N:15][O:16][CH3:17])[C:12]([NH:18][CH:19]2[C:39](=[O:40])[N:21]3[C:22]([C:26]([O:28][CH2:29][C:30]4[CH:31]=[CH:32][C:33]([N+:36]([O-:38])=[O:37])=[CH:34][CH:35]=4)=[O:27])=[CH:23][CH2:24][S:25][C@H:20]23)=[O:14])[N:8]=[N:7]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 5

HCID 24813Phosphorus oxychlorideHCID 357676Acetamide, 2-(trimethylsilyl)-HCID 11708267BistrimethylsilylacetamidHCID 12775080p-Nitrobenzyl 7-amino-3-cephem-4-carboxylateHCID 543473402-Methoxyimino-2-(1,2,3-thiadiazol-4-yl)acetic acid

生成物 2

HCID 77311Chloro-N,N-dimethylformiminium chloride
HCID 131712449p-Nitrobenzyl 7-{2-(1,2,3-thiadiazol-4-yl)-2-methoxyiminoacetamido}-3-cephem-4-carboxylate収率 168.4%

試薬・触媒・溶媒 3

HCID 962Water溶媒HCID 6228Dimethylformamide溶媒HCID 8857Ethyl Acetate溶媒3 回

実験手順

A solution of Vilsmeier reagent was prepared from dry dimethylformamide (0.39 g.), dry ethyl acetate (1.2 ml.) and phosphorus oxychloride (0.84 g.) in a usual manner. To the solution was added a solution of 2-(1,2,3-thiadiazol-4-yl)-2-methoxyiminoacetic acid (syn isomer, 0.93 g.) in ethyl acetate (10 ml.) at -15° C. to prepare the activated acid solution. On the other hand, a p-nitrobenzyl 7-amino-3-cephem-4-carboxylate (1.5 g.), trimethylsilylacetamide (4.6 g.) and bis(trimethylsilyl)acetamide (1 ml.) in dry ethyl acetate (50 ml.) was stirred at 45° C. for 5 hours to give a solution. To the solution was added all at once the activated acid solution obtained above at -10° C. with stirring, and the mixed solution was stirred at -5° C. for 1.5 hours. Water was added to the reaction mixture, and the insoluble product was separated by filtration, washed with ethyl acetate and water in turn, and then dried to give pale yellow powder of p-nitrobenzyl 7-{2-(1,2,3-thiadiazol-4-yl)-2-methoxyiminoacetamido}-3-cephem-4-carboxylate (syn isomer, 1.9 g.), m.p. 243° to 245° C. (dec.).

後処理

  1. customto prepare the activated acid solution
  2. customto give a solution
  3. additionTo the solution was added all at once the activated acid solution
  4. customobtained above at -10° C.
  5. stirringthe mixed solution was stirred at -5° C. for 1.5 hours
  6. customthe insoluble product was separated by filtration
  7. washwashed with ethyl acetate and water in turn
  8. customdried

出典と根拠

ORDレコード
ord-6af656038e0d40cfa198b7a5a78d275f
出典データセット
uspto-grants-1986_08
DOI
10.6084/m9.figshare.5104873.v1
特許番号
US04604456

反応ノート

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