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Tert-butyl 2-((7-(4-morpholinophenyl)pyrido[4,3-b]pyrazin-5-ylamino)methyl)-1,1-dioxo-thiomorpholine-4-carboxylate → 7-(4-morpholinophenyl)-N-(1,1-dioxo-thiomorpholin-2-ylmethyl)pyrido[4,3-b]pyrazin-5-amine

HRID 57649
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HRID 57649 반응식
[O:1]1[CH2:6][CH2:5][N:4]([C:7]2[CH:12]=[CH:11][C:10]([C:13]3[N:22]=[C:21]([NH:23][CH2:24][CH:25]4[S:30](=[O:32])(=[O:31])[CH2:29][CH2:28][N:27](C(OC(C)(C)C)=O)[CH2:26]4)[C:20]4[C:15](=[N:16][CH:17]=[CH:18][N:19]=4)[CH:14]=3)=[CH:9][CH:8]=2)[CH2:3][CH2:2]1>Cl.C(OCC)(=O)C>[O:1]1[CH2:6][CH2:5][N:4]([C:7]2[CH:8]=[CH:9][C:10]([C:13]3[N:22]=[C:21]([NH:23][CH2:24][CH:25]4[S:30](=[O:32])(=[O:31])[CH2:29][CH2:28][NH:27][CH2:26]4)[C:20]4[C:15](=[N:16][CH:17]=[CH:18][N:19]=4)[CH:14]=3)=[CH:11][CH:12]=2)[CH2:3][CH2:2]1
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참가 물질

4

반응물 1

HCID 86717408Tert-butyl 2-((7-(4-morpholinophenyl)pyrido[4,3-b]pyrazin-5-ylamino)methyl)-1,1-dioxo-thiomorpholine-4-carboxylate

생성물 1

HCID 867174097-(4-morpholinophenyl)-N-(1,1-dioxo-thiomorpholin-2-ylmethyl)pyrido[4,3-b]pyrazin-5-amine수율 77.2%

시약·촉매·용매 2

HCID 313Hydrochloric Acid용매HCID 8857Ethyl Acetate용매

실험 절차

The tert-butyl 2-((7-(4-morpholinophenyl)pyrido[4,3-b]pyrazin-5-ylamino)methyl)-1,1-dioxo-thiomorpholine-4-carboxylate (52 mg, 0.094 mmol) was dissolved in the solution of HCl in ethyl acetate (3 mL), and the mixture was stirred at room temperature for 2 hours until TLC indicated Boc group was removed. The volatile materials was removed, the residue was neutralized with ammonium hydroxide (25%, 1 mL) and purified by C18 column to afford yellow solid 33 mg. MS (m/z): 455 (M+H)+

후처리

  1. customwas removed
  2. customThe volatile materials was removed
  3. custompurified by C18 column

출처 및 근거

ORD 기록
ord-1a7876c106914f51b5faabb6ad118692
출처 데이터셋
uspto-grants-2016_09
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US09434726B2

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