Hydrochloric Acid → N-((5,5-difluoropiperidin-3-yl)methyl)-7-(4-morpholinophenyl)pyrido[4,3-b]pyrazin-5-amine

HRID 57615

反応式

HRID 57615 の反応式
[F:1][C:2]1([F:39])[CH2:7][CH:6]([CH2:8][NH:9][C:10]2[C:19]3[C:14](=[N:15][CH:16]=[CH:17][N:18]=3)[CH:13]=[C:12]([C:20]3[CH:25]=[CH:24][C:23]([N:26]4[CH2:31][CH2:30][O:29][CH2:28][CH2:27]4)=[CH:22][CH:21]=3)[N:11]=2)[CH2:5][N:4](C(OC(C)(C)C)=O)[CH2:3]1.Cl>>[F:39][C:2]1([F:1])[CH2:3][NH:4][CH2:5][CH:6]([CH2:8][NH:9][C:10]2[C:19]3[C:14](=[N:15][CH:16]=[CH:17][N:18]=3)[CH:13]=[C:12]([C:20]3[CH:21]=[CH:22][C:23]([N:26]4[CH2:27][CH2:28][O:29][CH2:30][CH2:31]4)=[CH:24][CH:25]=3)[N:11]=2)[CH2:7]1

参加物

3

反応物 2

HCID 313Hydrochloric AcidHCID 71113804Tert-butyl 3,3-difluoro-5-((7-(4-morpholinophenyl)pyrido[4,3-b]pyrazin-5-ylamino)methyl)piperidine-1-carboxylate

生成物 1

HCID 71113816N-((5,5-difluoropiperidin-3-yl)methyl)-7-(4-morpholinophenyl)pyrido[4,3-b]pyrazin-5-amine

実験手順

tert-Butyl 3,3-difluoro-5-((7-(4-morpholinophenyl)pyrido[4,3-b]pyrazin-5-ylamino)methyl)piperidine-1-carboxylate from step A (227 mg, 0.42 mmol) was treated with HCl solution (in EtOAc, 5 N) at room temperature until the reaction was finished. The volatiles were removed under reduced pressure, dissolved in dichloromethane (5 mL), and neutralized with ammonium hydroxide. The dichloromethane phase was concentrated to afford N-((5,5-difluoropiperidin-3-yl)methyl)-7-(4-morpholinophenyl)pyrido[4,3-b]pyrazin-5-amine. MS (m/z): 441 (M+H)+.

後処理

  1. customThe volatiles were removed under reduced pressure
  2. dissolutiondissolved in dichloromethane (5 mL)
  3. concentrationThe dichloromethane phase was concentrated

出典と根拠

ORDレコード
ord-75b30ea9a5ba40a6bc265c2846b58848
出典データセット
uspto-grants-2016_09
特許番号
US09434726B2

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