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Maleic Acid → Prasugrel (Maleic acid)

HRID 2120713
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HRID 2120713 반응식
[C:1]([OH:8])(=[O:7])/[CH:2]=[CH:3]\[C:4]([OH:6])=[O:5].[C:9]([O:12][C:13]1[S:21][C:20]2[CH2:19][CH2:18][N:17]([CH:22]([C:30]([CH:32]3[CH2:34][CH2:33]3)=[O:31])[C:23]3[CH:28]=[CH:27][CH:26]=[CH:25][C:24]=3[F:29])[CH2:16][C:15]=2[CH:14]=1)(=[O:11])[CH3:10]>CC(C)=O>[C:1]([OH:8])(=[O:7])/[CH:2]=[CH:3]\[C:4]([OH:6])=[O:5].[C:9]([O:12][C:13]1[S:21][C:20]2[CH2:19][CH2:18][N:17]([CH:22]([C:30]([CH:32]3[CH2:34][CH2:33]3)=[O:31])[C:23]3[CH:28]=[CH:27][CH:26]=[CH:25][C:24]=3[F:29])[CH2:16][C:15]=2[CH:14]=1)(=[O:11])[CH3:10]
참가 물질반응 조건실험 절차후처리출처 및 근거반응 노트

참가 물질

4

반응물 2

HCID 444266Maleic AcidHCID 6918456Prasugrel

생성물 1

HCID 9870150Prasugrel (Maleic acid)수율 92%

시약·촉매·용매 1

HCID 180Acetone용매

반응 조건

온도
25 °C

실험 절차

To a solution of maleic acid (4.43 g) in acetone (60 ml) was added 2-acetoxy-5-(α-cyclopropylcarbonyl-2-fluorobenzyl)-4,5,6,7-tetrahydrothieno[3,2-c]pyridine (15.0 g) obtained in Reference example 1, then the mixture was stirred at room temperature (25° C.) for 2 hours. The resulting crystals were separated by filtration and washed with a small amount of acetone and then dried at 50° C. under reduced pressure for 4 hours to give the title compound as white crystals (17.1 g, yield 92%)

후처리

  1. customobtained in Reference example 1
  2. customThe resulting crystals were separated by filtration
  3. washwashed with a small amount of acetone
  4. customdried at 50° C. under reduced pressure for 4 hours

출처 및 근거

ORD 기록
ord-6f2a7f9e76894af28dbc1505340248eb
출처 데이터셋
uspto-grants-2004_02
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US06693115B2

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