Cesium fluoride → HCID 70979030、化合物

HRID 1852145ノート

反応式

HRID 1852145 の反応式
Cl[C:2]1[C:11]2[C:6](=[CH:7][C:8]([O:12][CH3:13])=[CH:9][CH:10]=2)[C:5]([O:14][CH2:15][CH2:16][O:17][CH3:18])=[CH:4][N:3]=1.[F-:19].[Cs+]>CS(C)=O>[F:19][C:2]1[C:11]2[C:6](=[CH:7][C:8]([O:12][CH3:13])=[CH:9][CH:10]=2)[C:5]([O:14][CH2:15][CH2:16][O:17][CH3:18])=[CH:4][N:3]=1

参加物

4

反応条件

温度
140 °C

実験手順

To a solution of 1-chloro-6-methoxy-4-(2-methoxyethoxy)isoquinoline (560 mg, 2.092 mmol) in DMSO (5 mL) was added CsF (636 mg, 4.18 mmol) and heated to 140° C. for 2 hrs. LC/MS showed the desired product. The reaction was diluted with Ethylacteate and washed with water, and brine. The organic phase was collected, dried over MgSO4, and concentrated under vacuum to give the crude product as a reddish brown solid. The crude material was purified via silica gel chromatography (5-50% EtOAc:Hex) to give the product 1-fluoro-6-methoxy-4-(2-methoxyethoxy)isoquinoline (168 mg, 0.669 mmol, 32.0% yield) as a light yellow solid. MS: MS m/z 252.2(M++1).

出典と根拠

ORDレコード
ord-082647355cdb473eb94eadf48793f308
出典データセット
uspto-grants-2015_02
特許番号
US08957203B2

反応ノート

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