|EUTICALS S.P.A. Patent applications|
|Patent application number||Title||Published|
|20130178644||PROCESS FOR THE SYNTHESIS OF TAPENTADOL AND INTERMEDIATES THEREOF - The object of the present invention is a new process for the synthesis of tapentadol, both as free base and in hydrochloride form, which comprises the step of alkylation of the ketone (VII) to yield the compound (VIII), as reported in Diagram 1, with high stereoselectivity due to the presence of the benzyl group as substituent of the amino group. It was surprisingly found that this substitution shifts the keto-enol equilibrium towards the desired enantiomer and amplifies the capacity of the stereocenter present in the compound (VII) to orient the nucleophilic addition of the organometallic compound at the carbonyl towards the desired stereoisomer. This substitution thus allows obtaining a considerable increase of the yields in this step, and consequently allows significantly increasing the overall yield of the entire tapentadol synthesis process.||07-11-2013|
|20130030216||PROCESS FOR THE PREPARATION OF LACOSAMIDE - A novel process for the synthesis of Lacosamide using D,L-serine as starting material is described, where the methylation reaction of hydroxyl is carried out using an inexpensive base such as NaOH and an inexpensive alkylating agent, non-toxic and non-carcinogenic, such as methyl p-toluenesulfonate; the R enantiomer is isolated from the racemic mixture of Lacosamide after selective hydrolysis of the acetamide, salification of the racemic mixture with a chiral acid (HX*) in an organic solvent, resolution of the diastereoisomeric mixture, preferably by precipitation of the R enantiomer, and subsequent acetylation of the optically pure intermediate.||01-31-2013|
|20120232306||PROCESS FOR THE PREPARATION OF TAPENTADOL AND INTERMEDIATES THEREOF - The present invention refers to a new process for the synthesis of tapentadol comprising the quantitative resolution of the racemic mixture (V) to obtain the stereoisomer of (S)-3-(dimethylamino)-2-methyl-1-(3-nitrophenyl)-propan-1-one (VII) according to the Scheme 2 below||09-13-2012|
|20100035796||17-ALPHA-SUBSTITUTED DERIVATIVES OF ESTRADIOL WITH WOUND-HEALING ACTIVITY - The invention relates to 17α-(5-hydroxy-C||02-11-2010|
Patent applications by EUTICALS S.P.A.