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Hydrochloric Acid → N-[(3R)-1-(Aminoacetyl)piperidin-3-yl]-6-pyrazolo[1,5-a]pyridin-3-ylpyrazin-2-amine

HRID 1500783
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HRID 1500783 반응식
Cl.[O:2]=[C:3]([N:13]1[CH2:18][CH2:17][CH2:16][C@@H:15]([NH:19][C:20]2[CH:25]=[N:24][CH:23]=[C:22]([C:26]3[CH:27]=[N:28][N:29]4[CH:34]=[CH:33][CH:32]=[CH:31][C:30]=34)[N:21]=2)[CH2:14]1)[CH2:4][NH:5]C(=O)OC(C)(C)C>O1CCOCC1.CO>[NH2:5][CH2:4][C:3]([N:13]1[CH2:18][CH2:17][CH2:16][C@@H:15]([NH:19][C:20]2[CH:25]=[N:24][CH:23]=[C:22]([C:26]3[CH:27]=[N:28][N:29]4[CH:34]=[CH:33][CH:32]=[CH:31][C:30]=34)[N:21]=2)[CH2:14]1)=[O:2]
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참가 물질

5

반응물 2

HCID 313Hydrochloric AcidHCID 86691788Tert-Butyl (2-oxo-2-{(3R)-3-[(6-pyrazolo[1,5-a]pyridin-3-ylpyrazin-2-yl)amino]piperidin-1-yl}ethyl)carbamate

생성물 1

HCID 53373775N-[(3R)-1-(Aminoacetyl)piperidin-3-yl]-6-pyrazolo[1,5-a]pyridin-3-ylpyrazin-2-amine수율 95%

시약·촉매·용매 2

HCID 887Methanol용매HCID 312751,4-Dioxane
용매

실험 절차

A solution of hydrochloric acid in dioxane (4M, 10 mL) was added to a solution of tert-butyl (2-oxo-2-{(3R)-3-[(6-pyrazolo[1,5-a]pyridin-3-ylpyrazin-2-yl)amino]piperidin-1-yl}ethyl)carbamate (Preparation 38, 88 mg, 0.23 mmol) in methanol (3 mL) and the resulting mixture was stirred at ambient temperature for one hour. The solvents were then evaporated to half of their volume and the yellow solid that precipitated was filtered, washed with diethyl ether and dried to give the title compound (76 mg, 95%).

후처리

  1. customThe solvents were then evaporated to half of their volume
  2. customthe yellow solid that precipitated
  3. filtrationwas filtered
  4. washwashed with diethyl ether
  5. customdried

출처 및 근거

ORD 기록
ord-2b61ceb6c94345158ab34b14284a0367
출처 데이터셋
uspto-grants-2015_12
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US09206183B2

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