F.i.s. Fabbrica Italiana Sintetici S.p.a.

Filippo Tomasi

Nicolas Tesson

Elena Brasola

Loris Peruzzi

Marco Galvagni

Siro Serafini

Montserrat Trilla Castaño

Object of the present invention are dimer impurities of the active ingredient Apixaban, analytical methods for identifying and/or quantifying them and a synthetic method for removing or limiting said impurities from Apixaban and synthetic precursors thereof.

Dimer impurities of Apixaban and method to remove them

Dimer impurities of apixaban and method to remove them

Object of the present invention is an improved process for the preparation of Apixaban, through new intermediates which undergo to a faster amidation reaction. Impurities of Apixaban are also identified and quantified.

Key intermediates and impurities of the synthesis of Apixaban: Apixaban glycol esters

Key intermediates and impurities of the synthesis of apixaban: apixaban glycol esters

The present invention relates to a process for the synthesis of quetiapine. In particular, a process is provided for the synthesis of quetiapine of formula (A) comprising reacting dibenzo[b,f][1,4]thiazepin-11(10H)-one, intermediate (I) with phosphorous oxychloride to give 11-chlorodibenzo[b,f][1,4]thiazepine, intermediate (II) wherein the said reaction of intermediate (I) to intermediate (II) is performed in an organic solvent in the presence of a mixture of an organic base together with an inorganic base. 

Process for the synthesis of quetiapine

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Brogliano, Italy

Filippo Tomasi