Water → N-(5-(pyrazin-2-yl)-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)acetamide

HRID 39362

반응식

HRID 39362 반응식
[N:1]1[C:9]2[CH2:8][CH2:7][NH:6][CH2:5][C:4]=2[S:3][C:2]=1[NH:10][C:11](=[O:13])[CH3:12].Cl[C:15]1[CH:20]=[N:19][CH:18]=[CH:17][N:16]=1.O>CN1C(=O)CCC1>[N:16]1[CH:17]=[CH:18][N:19]=[CH:20][C:15]=1[N:6]1[CH2:7][CH2:8][C:9]2[N:1]=[C:2]([NH:10][C:11](=[O:13])[CH3:12])[S:3][C:4]=2[CH2:5]1

참가 물질

5

반응물 3

HCID 962WaterHCID 73277ChloropyrazineHCID 28274565N-(4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)acetamide

생성물 1

HCID 46873663N-(5-(pyrazin-2-yl)-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)acetamide수율 9.7%

시약·촉매·용매 1

HCID 13387N-methyl-2-pyrrolidone용매

반응 조건

온도
250 °C

실험 절차

As shown in step 10-iv of Scheme 10, to a solution of 50 mg of Compound 1035 in 3 mL of NMP was added 100 mg of 2-chloro pyrazine. The reaction mixture was warmed to 250° C. for 10 minutes under microwave irradiation. The reaction was poured into water (10 mL) and the crude product collected by filtration. The crude solid was purified by silica gel chromatography (CH2Cl2 to EtOH) to provide N-(5-(pyrazin-2-yl)-4,5,6,7-tetrahydrothiazolo[5,4-c]pyridin-2-yl)acetamide (Compound 1, 6.8 mg): ESMS (M+H) 276.16.

후처리

  1. filtrationthe crude product collected by filtration
  2. customThe crude solid was purified by silica gel chromatography (CH2Cl2 to EtOH)

출처 및 근거

ORD 기록
ord-33e117da437743818d6eadef14513599
출처 데이터셋
uspto-grants-2013_09
특허 번호
US08524906B2

연결된 노트

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