Hydrochloric Acid → 1-[4-(9-Fluoro-3-phenylpyrimido[1,2-b]indazole-2-yl)phenyl]-cyclobutylamine

HRID 877052ノート

反応式

HRID 877052 の反応式
C(OC(=O)[NH:7][C:8]1([C:12]2[CH:17]=[CH:16][C:15]([C:18]3[C:31]([C:32]4[CH:37]=[CH:36][CH:35]=[CH:34][CH:33]=4)=[CH:30][N:21]4[N:22]=[C:23]5[C:28]([CH:27]=[C:26]([F:29])[CH:25]=[CH:24]5)=[C:20]4[N:19]=3)=[CH:14][CH:13]=2)[CH2:11][CH2:10][CH2:9]1)(C)(C)C.Cl>O1CCOCC1>[F:29][C:26]1[CH:25]=[CH:24][C:23]2[C:28](=[C:20]3[N:19]=[C:18]([C:15]4[CH:14]=[CH:13][C:12]([C:8]5([NH2:7])[CH2:9][CH2:10][CH2:11]5)=[CH:17][CH:16]=4)[C:31]([C:32]4[CH:33]=[CH:34][CH:35]=[CH:36][CH:37]=4)=[CH:30][N:21]3[N:22]=2)[CH:27]=1

参加物

4

反応物 2

HCID 313Hydrochloric AcidHCID 86702529{1-[4-(9-Fluoro-3-phenylpyrimido[1,2-b]indazole-2-yl)phenyl]cyclobutyl}carbamic acid tert-butyl ester

生成物 1

HCID 573777651-[4-(9-Fluoro-3-phenylpyrimido[1,2-b]indazole-2-yl)phenyl]-cyclobutylamine収率 38.2%

試薬・触媒・溶媒 1

HCID 312751,4-Dioxane溶媒2 回

実験手順

In a second experiment 420 mg (0.83 mmol) {1-[4-(9-fluoro-3-phenylpyrimido[1,2-b]indazole-2-yl)phenyl]cyclobutyl}carbamic acid tert-butyl ester, after dissolution in 5 mL dioxane, were treated with 22 mL 4M hydrogen chloride in dioxane. The reaction mixture was worked up as described for the first experiment. The crude products of both experiments were purified by joint chromatography on amine silicagel (eluents: dichoromethane/methanol) yielding 129.5 mg of the desired product.

後処理

  1. customThe crude products of both experiments were purified by joint chromatography on amine silicagel (eluents: dichoromethane/methanol)

出典と根拠

ORDレコード
ord-591650d5eb1047fdb392c2f6e2e604ce
出典データセット
uspto-grants-2015_03
特許番号
US08987286B2

反応ノート

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