1-(2-Fluoroethyl)-3-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)urea → (S)-1-(2-fluoroethyl)-3-(4-(4-(3-methylmorpholino)pyrimidin-2-yl)phenyl)urea

HRID 1771563ノート

反応式

HRID 1771563 の反応式
Cl[C:2]1[N:7]=[C:6]([N:8]2[CH2:13][CH2:12][O:11][CH2:10][C@@H:9]2[CH3:14])[CH:5]=[CH:4][N:3]=1.[F:15][CH2:16][CH2:17][NH:18][C:19]([NH:21][C:22]1[CH:27]=[CH:26][C:25](B2OC(C)(C)C(C)(C)O2)=[CH:24][CH:23]=1)=[O:20]>>[F:15][CH2:16][CH2:17][NH:18][C:19]([NH:21][C:22]1[CH:27]=[CH:26][C:25]([C:2]2[N:7]=[C:6]([N:8]3[CH2:13][CH2:12][O:11][CH2:10][C@@H:9]3[CH3:14])[CH:5]=[CH:4][N:3]=2)=[CH:24][CH:23]=1)=[O:20]

参加物

3

反応物 2

HCID 446073531-(2-Fluoroethyl)-3-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)urea2 回HCID 72942067(S)-4-(2-Chloropyrimidin-4-yl)-3-methylmorpholine2 回

生成物 1

HCID 53379665(S)-1-(2-fluoroethyl)-3-(4-(4-(3-methylmorpholino)pyrimidin-2-yl)phenyl)urea

実験手順

Method as described for example 49 using (S)-4-(2-chloropyrimidin-4-yl)-3-methylmorpholine (intermediate 3) and 1-(2-fluoroethyl)-3-(4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)urea (intermediate 19). The mixture was purified by prep HPLC at high pH to afford the title compound. (15 mg, 9%).

後処理

  1. customThe mixture was purified by prep HPLC at high pH

出典と根拠

ORDレコード
ord-f972ad3ccf52401e9347e5dc13910736
出典データセット
uspto-grants-2016_02
特許番号
US09249129B2

反応ノート

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