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Hydrochloric Acid → 5-(1-(6-(1,4-diazepan-1-yl)pyridin-2-yl)-1H-pyrazolo[4,3-c]pyridin-6-yl)-3-methylpyrazin-2-amine

HRID 57913
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HRID 57913 반응식
[NH2:1][C:2]1[N:3]=[CH:4][C:5]([C:9]2[N:14]=[CH:13][C:12]3[CH:15]=[N:16][N:17]([C:18]4[N:23]=[C:22]([N:24]5[CH2:30][CH2:29][CH2:28][N:27](C(OC(C)(C)C)=O)[CH2:26][CH2:25]5)[CH:21]=[CH:20][CH:19]=4)[C:11]=3[CH:10]=2)=[N:6][C:7]=1[CH3:8].Cl>CO.O1CCOCC1>[N:24]1([C:22]2[N:23]=[C:18]([N:17]3[C:11]4[CH:10]=[C:9]([C:5]5[N:6]=[C:7]([CH3:8])[C:2]([NH2:1])=[N:3][CH:4]=5)[N:14]=[CH:13][C:12]=4[CH:15]=[N:16]3)[CH:19]=[CH:20][CH:21]=2)[CH2:30][CH2:29][CH2:28][NH:27][CH2:26][CH2:25]1
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참가 물질

5

반응물 2

HCID 313Hydrochloric AcidHCID 86707104Tert-butyl 4-[6-[6-(5-amino-6-methyl-pyrazin-2-yl)pyrazolo[4,3-c]pyridin-1-yl]-2-pyridyl]-1,4-diazepane-1-carboxylate

생성물 1

HCID 727143845-(1-(6-(1,4-diazepan-1-yl)pyridin-2-yl)-1H-pyrazolo[4,3-c]pyridin-6-yl)-3-methylpyrazin-2-amine수율 4.3%

시약·촉매·용매 2

HCID 887Methanol용매HCID 31275
1,4-Dioxane
용매

실험 절차

To a solution of tert-butyl 4-[6-[6-(5-amino-6-methyl-pyrazin-2-yl)pyrazolo[4,3-c]pyridin-1-yl]-2-pyridyl]-1,4-diazepane-1-carboxylate (0.2293 mmol; 115 mg) in Methanol (10 mL) was added hydrochloric acid, 4.0 M in 1,4-Dioxane (5 mL). The resulting mixture was stirred at room temperature overnight. The mixture was concentrated and the residue was purified by reverse phase HPLC to afford 208 as an off-white solid (4.0 mg, 4.3%). MS (ESI) m/z: 402.1 [M+H]+

후처리

  1. concentrationThe mixture was concentrated
  2. customthe residue was purified by reverse phase HPLC

출처 및 근거

ORD 기록
ord-494d52cf1bef42c79b1c307f0482524b
출처 데이터셋
uspto-grants-2016_09
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US09434725B2

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