Zeng Zhi-xua
2015
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Journal
Chemical Research and Application
Abstract
Ticagrelor was synthesized from 4,6-dichloro-2-( propylthio)-5-pyrimidinamine( 3) and 2-{ [( 3aR,4S,6R,6a S)-6-amino-2,2-dimethyltetrahydro-3a H-cyclopenta[d][1,3]-dioxol-4-yl]oxy}-1-ethanol,L-tartrate acid salt( 4) by nucleophileic substitution,cyclization and then reacting with( 1R,2S)-2-( 3,4-difluorophenyl) cyclopropylamine,D-mandelic acid salt( 2),followed by deprotection with diluted hydrochloric acid. The target compound was confirmed by1 H NMR and MS and the overall yield was 65%.