AMD070, a CXCR4 Chemokine Receptor Antagonist: Practical Large-Scale Laboratory Synthesis
作者： Jason B. Crawford , Gang Chen , David Gauthier , Trevor Wilson , Bryon Carpenter
DOI: 10.1021/OP8000993
关键词:
摘要: An efficient and convergent four-step synthetic route to the CXCR4 chemokine receptor antagonist AMD070 (1) has been developed which employs only a single chromatographic step in entire sequence. Novel reductive amination methods have for coupling of 2 3 dehydrative imine formation is followed by reduction with an attenuated borohydride reagent (zinc chloride sodium borohydride). Selective extraction were employed purify intermediates remove reagents impurities. A procedure also isolate 1 pure crystalline form.
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