Water → Atorvastatin

HRID 71008

반응식

HRID 71008 반응식
[CH3:1][CH:2]([C:4]1[N:8]([CH2:9][CH2:10][C@@H:11]([OH:19])[CH2:12][C@@H:13]([OH:18])[CH2:14][C:15]([OH:17])=[O:16])[C:7]([C:20]2[CH:21]=[CH:22][C:23]([F:26])=[CH:24][CH:25]=2)=[C:6]([C:27]2[CH:28]=[CH:29][CH:30]=[CH:31][CH:32]=2)[C:5]=1[C:33]([NH:35][C:36]1[CH:37]=[CH:38][CH:39]=[CH:40][CH:41]=1)=[O:34])[CH3:3].[OH-].[NH4+:43].O>C(#N)C>[CH3:3][CH:2]([C:4]1[N:8]([CH2:9][CH2:10][C@@H:11]([OH:19])[CH2:12][C@@H:13]([OH:18])[CH2:14][C:15]([OH:17])=[O:16])[C:7]([C:20]2[CH:25]=[CH:24][C:23]([F:26])=[CH:22][CH:21]=2)=[C:6]([C:27]2[CH:32]=[CH:31][CH:30]=[CH:29][CH:28]=2)[C:5]=1[C:33]([NH:35][C:36]1[CH:41]=[CH:40][CH:39]=[CH:38][CH:37]=1)=[O:34])[CH3:1].[NH4+:43].[F:26][C:23]1[CH:22]=[CH:21][C:20]([C:7]2[N:8]([CH2:9][CH2:10][CH:11]([OH:19])[CH2:12][CH:13]([OH:18])[CH2:14][C:15]([O-:17])=[O:16])[C:4]([CH:2]([CH3:3])[CH3:1])=[C:5]([C:33]([NH:35][C:36]3[CH:37]=[CH:38][CH:39]=[CH:40][CH:41]=3)=[O:34])[C:6]=2[C:27]2[CH:28]=[CH:29][CH:30]=[CH:31][CH:32]=2)=[CH:25][CH:24]=1

참가 물질

6

반응물 3

HCID 962WaterHCID 14923Ammonium HydroxideHCID 60823Atorvastatin2회

생성물 2

HCID 60823AtorvastatinHCID 730592022-(4-Fluorophenyl)-beta,delta-dihydroxy-5-(1-methylethyl)-3-phenyl-4-[(phenylamino)carbonyl]-1H-pyrrole-1-heptanoic acid, ammonium salt

시약·촉매·용매 1

HCID 6342Acetonitrile용매3회

실험 절차

The ammonium salt of atorvastatin was synthesized by preparing a stock solution of the free acid of atorvastatin (U.S. Pat. No. 5,273,995) in acetonitrile (ACN) (0.634 g in 25 mL of ACN). A solution was prepared by dissolving 12.04 mg of ammonium hydroxide (1.0 equivalents) in acetonitrile (0.5 mL). The stock solution of atorvastatin free acid (2.24 mL) was added to the counterion solution with stirring. If a gel formed, additional acetonitrile and water was added as necessary. After 2 days of stirring at ambient temperature, the solids were isolated by vacuum filtration using a 0.45 μm nylon 66 membrane filter. The solids were rinsed with acetonitrile and air dried at ambient conditions to afford atorvastatin ammonium.

후처리

  1. customA solution was prepared
  2. customIf a gel formed
  3. stirringAfter 2 days of stirring at ambient temperature
  4. customthe solids were isolated by vacuum filtration
  5. filtrationfilter
  6. washThe solids were rinsed with acetonitrile and air
  7. customdried at ambient conditions

출처 및 근거

ORD 기록
ord-9e2499e4b83b4abe811afdfbf3734ae0
출처 데이터셋
uspto-grants-2014_09
특허 번호
US08822703B2

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