Ammonia → 5-Amino-7-(3-amino-3-methyl1-pyrrolidinyl)-1-cyclopropyl-6,8-difluoro-1,4-dihydro4-oxoquinoline-3-carboxylic acid

HRID 477026노트

반응식

HRID 477026 반응식
[NH2:1][C:2]1([CH3:27])[CH2:6][CH2:5][N:4]([C:7]2[C:16]([F:17])=[C:15]3[C:10]([C:11](=[O:24])[C:12]([C:21]([OH:23])=[O:22])=[CH:13][N:14]3[CH:18]3[CH2:20][CH2:19]3)=[C:9](F)[C:8]=2[F:26])[CH2:3]1.[NH3:28]>>[NH2:28][C:9]1[C:8]([F:26])=[C:7]([N:4]2[CH2:5][CH2:6][C:2]([NH2:1])([CH3:27])[CH2:3]2)[C:16]([F:17])=[C:15]2[C:10]=1[C:11](=[O:24])[C:12]([C:21]([OH:23])=[O:22])=[CH:13][N:14]2[CH:18]1[CH2:19][CH2:20]1

참가 물질

3

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온도
100 °C

실험 절차

A mixture of 7-(3-amino-3-methyl-1-pyrrolidinyl)-1-cyclopropyl-5,6,8-trifluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid (150 mg) and 28% aqueous ammonia (15 ml) was heated at 100° C. for 48 hours in a sealed tube. The reaction mixture was evaporated to dryness under reduced pressure and water was added to the residue. The resulting crystals were treated in the same manner as described in Example 10 (1) to give 5-amino7-(3-amino-3-methyl-1-pyrrolidinyl)-1-cyclopropyl-6,8-difluoro-1,4-dihydro-4-oxoquinoline-3-carboxylic acid (93 mg), m.p. 271°-273° C (decomp.).

후처리

  1. customThe reaction mixture was evaporated to dryness under reduced pressure and water
  2. additionwas added to the residue
  3. additionThe resulting crystals were treated in the same manner

출처 및 근거

ORD 기록
ord-21fb80f8f9384f09a84f946faa05538b
출처 데이터셋
uspto-grants-1989_12
특허 번호
US04886810

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