Acetone → Tamiflu

HRID 15608

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HRID 15608 반응식
[CH3:1][CH2:2][CH:3]([O:6][C@H:7]1[C@H:12]([NH:13][C:14]([CH3:16])=[O:15])[C@@H:11]([NH2:17])[CH2:10][C:9]([C:18]([O:20][CH2:21][CH3:22])=[O:19])=[CH:8]1)[CH2:4][CH3:5].C(O)(C(O)=O)C(O)C(O)=O.CC(C)=O.[OH:37][P:38]([OH:41])([OH:40])=[O:39]>C(O)C>[CH3:5][CH2:4][CH:3]([O:6][C@H:7]1[C@H:12]([NH:13][C:14]([CH3:16])=[O:15])[C@@H:11]([NH2:17])[CH2:10][C:9]([C:18]([O:20][CH2:21][CH3:22])=[O:19])=[CH:8]1)[CH2:2][CH3:1].[OH:39][P:38]([OH:41])([OH:40])=[O:37]

참가 물질

5

반응물 3

HCID 180AcetoneHCID 1004Phosphoric AcidHCID 16667738Oseltamivir tartrate

생성물 1

HCID 78000Tamiflu수율 56.3%

시약·촉매·용매 1

HCID 702Ethanol용매

반응 조건

온도
27.5 °C

실험 절차

Oseltamivir tartrate (13 gm, obtained in example 3) is added to acetone (150 ml) at 25-30° C., the solution of H3PO4 (3.5 gm) in 40 ml of ethanol is added to the contents and then stirred for 1 hour 30 minutes at 25-30° C. Filtered the solid, washed with 30 ml of acetone and dried to yield 6.5 gm of oseltamivir phosphate (HPLC purity: 99.8%).

후처리

  1. filtrationFiltered the solid
  2. washwashed with 30 ml of acetone
  3. customdried

출처 및 근거

ORD 기록
ord-958f4ca71a0043ed81f947dbc750f7d2
출처 데이터셋
uspto-grants-2010_06
특허 번호
US07732632B2

연결된 노트

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