2-(3-Hydroxy-2-pyridyl)-4-thiazolecarboxylic acid → HCID 178522729、化合物

HRID 1638322ノート

反応式

HRID 1638322 の反応式
[OH:1][C:2]1[C:3]([C:8]2[S:9][CH:10]=[C:11]([C:13]([OH:15])=O)[N:12]=2)=[N:4][CH:5]=[CH:6][CH:7]=1.[NH2:16][C:17]1[NH:21][N:20]=[N:19][N:18]=1>CN(C=O)C>[OH:1][C:2]1[C:3]([C:8]2[S:9][CH:10]=[C:11]([C:13]([NH:16][C:17]3[NH:21][N:20]=[N:19][N:18]=3)=[O:15])[N:12]=2)=[N:4][CH:5]=[CH:6][CH:7]=1

参加物

4

反応物 2

HCID 1362052682-(3-Hydroxy-2-pyridyl)-4-thiazolecarboxylic acidHCID 178509299HCID 178509299、化合物

生成物 1

HCID 178522729HCID 178522729、化合物収率 54%

試薬・触媒・溶媒 1

HCID 6228Dimethylformamide溶媒2 回

反応条件

温度
80 °C

実験手順

A suspension of 2-(3-hydroxy-2-pyridyl)-4-thiazolecarboxylic acid (200 mg) and N,N'-carbonyldiimidazole (hereinafter, referred to as CDI) (291.9 mg) in dry DMF (7 ml), prepared under argon atmosphere, was heated at 80° C. for 1.5 hours. A solution of 5-aminotetrazole (91.9 mg) in dry DMF (3 ml) was added dropwise thereto and allowed to react at 85° C. for 3.5 hours. Then the reaction mixture was cooled to room temperature. The produced solids were filtered with suction, washed with DMF and THF and dried to give white solids of 2-(3-hydroxy-2-pyridyl)-N-(1H-tetrazole-5-yl)-4-thiazolecarboxamide (140 mg, 54%), m.p. above 300° C.

後処理

  1. customprepared under argon atmosphere
  2. customto react at 85° C. for 3.5 hours
  3. temperatureThen the reaction mixture was cooled to room temperature
  4. filtrationThe produced solids were filtered with suction
  5. washwashed with DMF and THF
  6. customdried

出典と根拠

ORDレコード
ord-c578c7d5c256459dac929f777e9b9349
出典データセット
uspto-grants-1989_11
特許番号
US04879295

反応ノート

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