Lamotrigine → Lamotrigine N-Acetate

HRID 1153712

반응식

HRID 1153712 반응식
[NH2:1][C:2]1[N:3]=[N:4][C:5]([C:9]2[CH:14]=[CH:13][CH:12]=[C:11]([Cl:15])[C:10]=2[Cl:16])=[C:6]([NH2:8])[N:7]=1.[C:17](OC(=O)C)(=[O:19])[CH3:18]>C(O)(=O)C>[C:17]([NH:8][C:6]1[N:7]=[C:2]([NH2:1])[N:3]=[N:4][C:5]=1[C:9]1[CH:14]=[CH:13][CH:12]=[C:11]([Cl:15])[C:10]=1[Cl:16])(=[O:19])[CH3:18]

참가 물질

4

반응물 2

HCID 3878LamotrigineHCID 7918Acetic Anhydride

생성물 1

HCID 23311124Lamotrigine N-Acetate

시약·촉매·용매 1

HCID 176Acetic Acid용매

실험 절차

A solution of 3,5-diamino-6-(2,3-dichlorophenyl)-1,2,4-triazine (2 gm, 8 mM) and acetic anhydride (10 mls) in acetic acid (20 mls) was stirred and heated to reflux for 2 hours. The solution was then cooled and evaporated down in vacuo. The residue was treated with aqueous 0.880 ammonia (100 mls) and the resultant mixture was stirred for 2 hours. The solid was separated by filtration, dried then recrystallized from isopropanol to give 5-acetamido-3-amino-6-(2,3-dichlorophenyl)-1,2,4-triazine. Yield 1.0 gms (42%), m.p. 250°-252° C. (uncorrected).

후처리

  1. temperatureheated
  2. temperatureto reflux for 2 hours
  3. temperatureThe solution was then cooled
  4. customevaporated down in vacuo
  5. additionThe residue was treated with aqueous 0.880 ammonia (100 mls)
  6. customThe solid was separated by filtration
  7. customdried
  8. customthen recrystallized from isopropanol

출처 및 근거

ORD 기록
ord-3c8ad30470454cc3891abd2ecd103bb3
출처 데이터셋
uspto-grants-1984_12
특허 번호
US04486354

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