2-(3-Hydroxy-2-pyridyl)-4-thiazolecarboxylic acid → HCID 178522729, 화합물

HRID 1638322노트

반응식

HRID 1638322 반응식
[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

참가 물질

4

반응물 2

HCID 1362052682-(3-Hydroxy-2-pyridyl)-4-thiazolecarboxylic acidHCID 178509299HCID 178509299, 화합물

생성물 1

HCID 178522729HCID 178522729, 화합물수율 54%

시약·촉매·용매 1

HCID 6228Dimethylformamide용매2회

반응 조건

온도
80 °C

실험 절차

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.

후처리

  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

출처 및 근거

ORD 기록
ord-c578c7d5c256459dac929f777e9b9349
출처 데이터셋
uspto-grants-1989_11
특허 번호
US04879295

반응 노트

불러오는 중…