Abstract: The present invention relates to a process for the preparation of aminoaryl- and aminoheteroaryl boronic acids and esters thereof of formula (I) in high yields starting from a dialkyl ketal derivative of formula (V)

Abstract: The present invention relates to a process for the preparation of aminoaryl- and aminoheteroaryl boronic acids and esters thereof of formula (I) in high yield. The claimed process uses diarylketal formula (V) to generate an arylbromide of formula (III) in which the amino-group is protected as bisarylmethylidenimino-group, which is then transformed into a formula (I) compound.

Abstract: 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.

Abstract: 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. A further object of the present invention is constituted by the tapentadol free base in solid form, obtainable by means of the process of the invention.

Abstract: Processes for preparing pimecrolimus starting from ascomycin, exploiting the selectivity characteristics of the purified enzymatic systems particularly regarding the selective functionalization of the hydroxyl groups present in position 24 and 33 of ascomycin. Such method represents the first example of chemoenzymatic synthesis for preparing pimecrolimus.

Abstract: 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 using the (2R,3R)—O,O?-dibenzoyltartaric chiral acid wherein said resolution is quantitative. The present invention also refers to some intermediate compounds of the new synthesis process of tapentadol.

Abstract: The invention relates to a procedure for stabilising polyunsaturated fatty acids with selective reducing agents. In particular, the invention relates to a process of preparation of polyunsaturated acids of the omega-3 series, as such or in the form of esters, which comprises treatment of fish oil or a mixture of acids with urea, and subsequent treatment with a metal hydride, preferably sodium borohydride. The polyunsaturated fatty acids of greatest interest present in fish oil are docosahexaenoic acid (DHA) and eicosapentaenoic acid (EPA).

Abstract: 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. A further object of the present invention is constituted by the tapentadol free base in solid form, obtainable by means of the process of the invention.

Abstract: 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.

Abstract: The invention relates to 17?-(5-hydroxy-C5-hydrocarbyl)-1,3,5(10)-estratrien-3,17?-diol derivatives having cicatrising activity, preferably for topical use on wounds, without significant systemic effects, and to pharmaceutical compositions containing them. In particular, the invention relates to estradiol 17?-(5-hydroxypentyn-1-yl)derivatives and 3-esters, 5?-esters and 3,5?-diesters thereof and to a process for the preparation thereof by reaction of 3-OR-protected estrone with an alkali metal derivative of OR-protected 5-pentynol, followed by 3-, 5-? or 3,5?-esterifÊcation.

Abstract: 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 using the (2R,3R)—O,O?-dibenzoyltartaric chiral acid wherein said resolution is quantitative. The present invention also refers to some intermediate compounds of the new synthesis process of tapentadol.

Abstract: A process for the preparation of 2-fluoroadenine with a purity of at least 98% (HPLC Area) is presented. Such very high purity degree of at least 98% (HPLC Area) is obtained directly on the crude product after reacting 2,6-diaminopurine in an amount of anhydrous fluorinating agent; heating the resulting reaction mixture; quenching the heated reaction mixture; separating the solid obtained thereby; and washing and separating the solid, without recrystallization and/or any further purification steps.

Abstract: The invention relates to 17?-(5-hydroxy-C5-hydrocarbyl)-1,3,5(10)-estratrien-3,17?-diol derivatives having cicatrising activity, preferably for topical use on wounds, without significant systemic effects, and to pharmaceutical compositions containing them. In particular, the invention relates to estradiol 17?-(5-hydroxypentyn-1-yl)derivatives and 3-esters, 5?-esters and 3,5?-diesters thereof and to a process for the preparation thereof by reaction of 3-OR-protected estrone with an alkali metal derivative of OR-protected 5-pentynol, followed by 3-, 5-? or 3,5?-esterification.

Abstract: A process for preparing pure L-alpha-Glycerylphosphoryl-D-Myoinositol and its salts consists of a) preparing the crude Na+ or K+ salt of L-.alpha.-Glycerylphosphoryl-D-Myoinositol, passing an aqueous solution of the salt through an acid resin in H form whereby ion exchange occurs and the acid L-.alpha.-Glycerylphosphoryl-D-Myoinositol is eluted by washing the resin with water. Then the aqueous solution is passed through a basic resin whereby the L-.alpha.-Glycerylphosphoryl-D-Myoinositol is adsorbed on the resin as the anion. The resin is eluted first with a dilute solution of formic, acetic or propionic acid and then eluted with a more concentrated solution of the same acid. The preparation of severals salts is also described.