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Hydrochloric Acid → (S)-1-(3-cyclopropyl-6-(6-(5-ethylpyridin-3-yl)-1H-pyrazolo[4,3-c]pyridin-1-yl)pyridin-2-yl)piperidin-3-amine

HRID 57837
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반응식

HRID 57837 반응식
[CH:1]1([C:4]2[C:5]([N:27]3[CH2:32][CH2:31][CH2:30][C@H:29]([NH:33]C(=O)OC(C)(C)C)[CH2:28]3)=[N:6][C:7]([N:10]3[C:18]4[CH:17]=[C:16]([C:19]5[CH:20]=[N:21][CH:22]=[C:23]([CH2:25][CH3:26])[CH:24]=5)[N:15]=[CH:14][C:13]=4[CH:12]=[N:11]3)=[CH:8][CH:9]=2)[CH2:3][CH2:2]1.Cl>CO.O1CCOCC1>[CH:1]1([C:4]2[C:5]([N:27]3[CH2:32][CH2:31][CH2:30][C@H:29]([NH2:33])[CH2:28]3)=[N:6][C:7]([N:10]3[C:18]4[CH:17]=[C:16]([C:19]5[CH:20]=[N:21][CH:22]=[C:23]([CH2:25][CH3:26])[CH:24]=5)[N:15]=[CH:14][C:13]=4[CH:12]=[N:11]3)=[CH:8][CH:9]=2)[CH2:3][CH2:2]1
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참가 물질

5

반응물 2

HCID 313Hydrochloric AcidHCID 86707042tert-butyl N-[(3S)-1-[3-cyclopropyl-6-[6-(5-ethyl-3-pyridyl)pyrazolo[4,3-c]pyridin-1-yl]-2-pyridyl]-3-piperidyl]carbamate

생성물 1

HCID 86707043(S)-1-(3-cyclopropyl-6-(6-(5-ethylpyridin-3-yl)-1H-pyrazolo[4,3-c]pyridin-1-yl)pyridin-2-yl)piperidin-3-amine수율 7.4%

시약·촉매·용매 2

HCID 887Methanol용매
HCID 31275
1,4-Dioxane
용매

실험 절차

To a solution of tert-butyl N-[(3S)-1-[3-cyclopropyl-6-[6-(5-ethyl-3-pyridyl)pyrazolo[4,3-c]pyridin-1-yl]-2-pyridyl]-3-piperidyl]carbamate (0.0597 mmol; 32.2 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 139 as an off-white solid (20 .mg, 7.4%). MS (ESI) m/z: 440.3 [M+H]+

후처리

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

출처 및 근거

ORD 기록
ord-8bc291c686de405dbbc482462a9bacb1
출처 데이터셋
uspto-grants-2016_09
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US09434725B2

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