HCID 66678959、化合物 → (S)-4-(6-chloro-2-(methylthio)pyrimidin-4-yl)-3-methylmorpholine

反応式

FC1C=C([C:8]2[N:13]=[C:12]([S:14][CH3:15])[N:11]=[C:10]([N:16]3[CH2:21][CH2:20][O:19][CH2:18][C@@H:17]3[CH3:22])[CH:9]=2)C=NC=1.[Cl:23]C1N=C(N2CCOC[C@@H]2C)C=C(C2C=NC=C(F)C=2)N=1.FC1C=C(NC(NCCO)=O)C=CC=1B1OC(C)(C)C(C)(C)O1>>[Cl:23][C:8]1[N:13]=[C:12]([S:14][CH3:15])[N:11]=[C:10]([N:16]2[CH2:21][CH2:20][O:19][CH2:18][C@@H:17]2[CH3:22])[CH:9]=1

参加物

反応物 3

HCID 66678959HCID 66678959、化合物2 回

HCID 67382782(S)-4-(6-(5-fluoropyridin-3-yl)-2-(methylthio)pyrimidin-4-yl)-3-methylmorpholine

HCID 86691143(S)-4-(2-chloro-6-(5-fluoropyridin-3-yl)pyrimidin-4-yl)-3-methylmorpholine2 回

生成物 1

HCID 86691142(S)-4-(6-chloro-2-(methylthio)pyrimidin-4-yl)-3-methylmorpholine収率 25%

実験手順

Method as described for intermediate 5 using (S)-4-(2-chloro-6-(5-fluoropyridin-3-yl)pyrimidin-4-yl)-3-methylmorpholine (intermediate 7) and 1-(3-fluoro-4-(4,4,5,5-tetramethyl-1,3,2-dioxaborolan-2-yl)phenyl)-3-(2-hydroxyethyl)urea (intermediate 13). Material was purified by prep HPLC (high pH) to afford a brown solid, (4 1 mg, 25%).