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(1R)-1-cyclopropylethan-1-amine hydrochloride → (R)-[4-(2-Chloro-4-dimethylamino-5-fluoro-phenyl)-3-nitro-pyridin-2-yl]-(1-cyclopropyl-ethyl)-amine

HRID 1831586
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반응식

HRID 1831586 반응식
OC(C(F)(F)F)=O.[Cl:8][C:9]1[CH:14]=[C:13]([N:15]([CH3:17])[CH3:16])[C:12]([F:18])=[CH:11][C:10]=1[C:19]1[CH:24]=[CH:23][N:22]=[C:21](OS(C(F)(F)F)(=O)=O)[C:20]=1[N+:33]([O-:35])=[O:34].Cl.[CH:37]1([C@H:40]([NH2:42])[CH3:41])[CH2:39][CH2:38]1>>[Cl:8][C:9]1[CH:14]=[C:13]([N:15]([CH3:17])[CH3:16])[C:12]([F:18])=[CH:11][C:10]=1[C:19]1[CH:24]=[CH:23][N:22]=[C:21]([NH:42][C@@H:40]([CH:37]2[CH2:39][CH2:38]2)[CH3:41])[C:20]=1[N+:33]([O-:35])=[O:34]
참가 물질실험 절차출처 및 근거반응 노트

참가 물질

3

반응물 2

HCID 55219897(1R)-1-cyclopropylethan-1-amine hydrochlorideHCID 131725817Trifluoro-methanesulfonic acid 4-(2-chloro-4-dimethylamino-5-fluoro-phenyl)-3-nitro-pyridin-2-yl ester TFA

생성물 1

HCID 69658051(R)-[4-(2-Chloro-4-dimethylamino-5-fluoro-phenyl)-3-nitro-pyridin-2-yl]-(1-cyclopropyl-ethyl)-amine수율 48.8%

실험 절차

Trifluoro-methanesulfonic acid 4-(2-chloro-4-dimethylamino-5-fluoro-phenyl)-3-nitro-pyridin-2-yl ester TFA (1.06 g, 2.49 mmol) and (R)-1-cyclopropyl-ethylamine HCl (202 mg, 1.7 mmol) were treated substantially as described in Part C of Example 19a to produce 314 mg of crude (R)-[4-(2-chloro-4-dimethylamino-5-fluoro-phenyl)-3-nitro-pyridin-2-yl]-(1-cyclopropyl-ethyl)-amine.

출처 및 근거

ORD 기록
ord-bff70a85e8244190a9e7b4fb9895b8fe
출처 데이터셋
uspto-grants-2006_06
DOI
10.6084/m9.figshare.5104873.v1
특허 번호
US07067658B2

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