Lamotrigine → 2-(2,3-Dichlorophenyl)-7-(1-quinolin-6-ylcyclopropyl)imidazo[1,2-b][1,2,4]triazin-3-amine

HRID 1257917

반응식

HRID 1257917 반응식
[Cl:1][C:2]1[C:7]([Cl:8])=[CH:6][CH:5]=[CH:4][C:3]=1[C:9]1[N:14]=[N:13][C:12]([NH2:15])=[N:11][C:10]=1[NH2:16].Cl[CH:18]([C:21]1([C:24]2[CH:25]=[C:26]3[C:31](=[CH:32][CH:33]=2)[N:30]=[CH:29][CH:28]=[CH:27]3)[CH2:23][CH2:22]1)[CH:19]=O>C(O)C>[Cl:1][C:2]1[C:7]([Cl:8])=[CH:6][CH:5]=[CH:4][C:3]=1[C:9]1[C:10]([NH2:16])=[N:11][C:12]2[N:13]([C:18]([C:21]3([C:24]4[CH:25]=[C:26]5[C:31](=[CH:32][CH:33]=4)[N:30]=[CH:29][CH:28]=[CH:27]5)[CH2:23][CH2:22]3)=[CH:19][N:15]=2)[N:14]=1

참가 물질

4

반응물 2

HCID 3878LamotrigineHCID 86621504Chloro(1-quinolin-6-ylcyclopropyl)acetaldehyde

생성물 1

HCID 594209862-(2,3-Dichlorophenyl)-7-(1-quinolin-6-ylcyclopropyl)imidazo[1,2-b][1,2,4]triazin-3-amine수율 35.3%

시약·촉매·용매 1

HCID 702Ethanol용매

반응 조건

온도
105 °C

실험 절차

A mixture of 6-(2,3-dichlorophenyl)-1,2,4-triazine-3,5-diamine (19 mg, 0.076 mmol) and chloro(1-quinolin-6-ylcyclopropyl)acetaldehyde (22 mg, 0.091 mmol) in ethanol (0.50 mL) was stirred at 105° C. overnight. The reaction mixture was purified by RP-HPLC (pH 10) to afford the desired product (12 mg, 35%). LCMS: (M+H)=447.3/449.2/451.2.

후처리

  1. customThe reaction mixture was purified by RP-HPLC (pH 10)

출처 및 근거

ORD 기록
ord-ff8d1570be5f45e5a4b5f2bad08afa2b
출처 데이터셋
uspto-grants-2013_06
특허 번호
US08461330B2

연결된 노트

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