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

HRID 877052노트

반응식

HRID 877052 반응식
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

참가 물질

4

반응물 2

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

생성물 1

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

시약·촉매·용매 1

HCID 312751,4-Dioxane용매2회

실험 절차

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.

후처리

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

출처 및 근거

ORD 기록
ord-591650d5eb1047fdb392c2f6e2e604ce
출처 데이터셋
uspto-grants-2015_03
특허 번호
US08987286B2

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