2013•Fine and Specialty ChemicalsRequires access
Synthesis of henatinib
Kong Shuang-hu
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Abstract
Beginning with 3,5-dimethyl-1H-pyrrole-2,4-dicarboxylic acid-2-tert-butyl ester 4-ethyl ester,the intermediate 6 was obtained after a series of oxidation,Wittig reaction,hydrogenation,hydrolysis,reduction and methyl sulfonylation reaction.After a nucleophilic substitution reaction between intermediate 6 and(S)-1-amino-3-morpholin-4-ylpropan-2-ol,the corresponding intermediate was treated with AlMe 3.After a formylation reaction,intermediate 9 was obtained.The final product henatinib was obtained after a reaction of intermediate 9 and 5-fluoro-1,3-dihydro-2H-indol2-one.