HCID 10903732, 화합물 → Lamivudine

HRID 1779330

반응식

HRID 1779330 반응식
[NH2:1][C:2]1[CH:7]=[CH:6][N:5]([C@H:8]2[O:12][C@@H:11]([CH2:13][O:14]C(=O)C3C=CC=CC=3)[S:10][CH2:9]2)[C:4](=[O:23])[N:3]=1>CO>[NH2:1][C:2]1[CH:7]=[CH:6][N:5]([C@H:8]2[O:12][C@@H:11]([CH2:13][OH:14])[S:10][CH2:9]2)[C:4](=[O:23])[N:3]=1

참가 물질

3

반응물 1

HCID 10903732HCID 10903732, 화합물2회

생성물 1

HCID 60825Lamivudine수율 90.4%

시약·촉매·용매 1

HCID 887Methanol용매

실험 절차

A suspension of (cis)-4-amino-1-(2-benzoyloxymethyl-1,3-oxathiolan-5-yl)(1H)-pyrimidin-2-one (Intermediate 3) (8.19 g) and Amberlite IRA-400 (OH) resin (8.24 g) in methanol (250 ml) was stirred and heated to reflux for 11/4 h. Solids were removed by filtration then washed with methanol. The combined filtrates were evaporated. The residue was triturated with ethyl acetate (80 ml). The resulting white solid was collected by filtration to give the title product (5.09 g), 1H NMR (DMSO-d6) 3.04 (1H), 3.40 (1H), 3.73 (2H), 5.18 (1H), 5.29 (1H), 5.73 (1H), 6.21 (1H), 7.19 (2H), 7,81 (1H).

후처리

  1. temperatureheated
  2. temperatureto reflux for 11/4 h
  3. customSolids were removed by filtration
  4. washthen washed with methanol
  5. customThe combined filtrates were evaporated
  6. customThe residue was triturated with ethyl acetate (80 ml)
  7. filtrationThe resulting white solid was collected by filtration

출처 및 근거

ORD 기록
ord-cdc06d0c6acb4738b9f849fb6fd5471a
출처 데이터셋
uspto-grants-1997_05
특허 번호
US05627186

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