Synthesis process of KX2-361-D4 benzene sulfonate

The invention belongs to the technical field of chemical synthesis, and particularly relates to a synthesis process of KX2-361-D4 benzene sulfonate. The invention relates to a synthesis process of KX2-361-D4 benzene sulfonate, which comprises the following steps: by taking a compound I 1, 4-dibromob...

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Hauptverfasser: LI GUOFENG, CUI TANGWU, WANG MINGQUAN, YANG WEIQIANG, JIA QI
Format: Patent
Sprache:chi ; eng
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Zusammenfassung:The invention belongs to the technical field of chemical synthesis, and particularly relates to a synthesis process of KX2-361-D4 benzene sulfonate. The invention relates to a synthesis process of KX2-361-D4 benzene sulfonate, which comprises the following steps: by taking a compound I 1, 4-dibromobenzene-D4 as a raw material, coupling with morpholine in the presence of Pd2 (dba) 3, BINAP and sodium tert-butoxide to obtain a deuterated intermediate 2, namely 4-(4-bromophenyl-2, 3, 5, 6-D4) morpholine; the preparation method comprises the following steps: preparing four deuterium-labeled KX2-361-D4 benzene sulfonate from four deuterium-labeled KX2-361-D4, sequentially carrying out Suzuki coupling, SNAr reaction, cyano hydrolysis reaction and amide condensation reaction to prepare KX2-361-D4, and finally salifying with benzenesulfonic acid to obtain the four deuterium-labeled KX2-361-D4 benzene sulfonate. The synthesis method of the KX2-361-D4 benzene sulfonate has the following technical effects that the synth