1437577-94-0Relevant articles and documents
An anti-thrombotic drug [...] method for the preparation of
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, (2017/03/08)
The invention discloses a preparation method of a compound Apixaban as an anti-thrombotic drug. The method disclosed by the invention comprises the following steps of: with a compound 11 shown as the formula 1 as a starting raw material, subjecting the compound 11 and amino protected paraiodoaniline 19 to coupling reaction in the existence of a cuprous reagent and an inorganic base to obtain a compound 20; subjecting the compound 20 and a compound 21 to [3+2] cyclization-elimination reaction to obtain a compound 22; removing a protecting group of the compound 22 to obtain a compound 23, or subjecting the compound 20 and the compound 21 to [3+2] cyclization reaction, directly carrying out elimination reaction under an acidic condition, and meanwhile, removing the protecting group to obtain the compound 23; subjecting the compound 23 to ammonolysis reaction to obtain a compound 24; subjecting the compound 24 and 5-chlorovaleryl halogen to amidation reaction to obtain a compound 25; and cyclizing the compound 25 under an alkaline condition to obtain the Apixaban, or subjecting the compound 24 and 5-chlorovaleryl bromine to amidation and cyclization two-step one-pot method reaction under the alkaline condition to obtain a target product, namely the Apixaban.
SOLID STATE FORMS OF APIXABAN
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, (2013/08/28)
The present invention is directed to solid state forms of Apixaban, processes for preparing the solid state forms, and pharmaceutical compositions thereof.