Abstract: The present invention relates to a process for preparing 3-amino tetrahydropyrans and, more particularly, to an improved method for synthesizing a 2,3,5-substituted tetrahydropyran derivative, intermediate being used in the preparation of dipeptidyl peptidase-IV enzyme inhibitors (DPP-4 inhibitors).

Abstract: The present invention relates to a process for preparing 3-amino tetrahydropyrans and, more particularly, to an improved method for synthesizing a 2,3,5-substituted tetrahydropyran derivative, intermediate being used in the preparation of dipeptidyl peptidase-IV enzyme inhibitors (DPP-4 inhibitors).

Abstract: The present invention relates to a process for the cyclopropanation with ethylene carbonate or ethylene sulfate of a compound of formula (II): wherein G is —CN or —COOR in which R is a C1-C4 straight or branched alkyl X and Y are independently selected from the group consisting of hydrogen, fluorine, chlorine, bromine, iodine, R1O— and R1S— wherein R1 is C1-C4 straight or branched alkyl chain.

Abstract: The present invention relates to a process for the cyclopropanation with ethylene carbonate or ethylene sulfate of a compound of formula (II): wherein G is —CN or —COOR in which R is a C1-C4 straight or branched alkyl X and Y are independently selected from the group consisting of hydrogen, fluorine, chlorine, bromine, iodine, R1O— and R1S— wherein R1 is C1-C4 straight or branched alkyl chain.

Abstract: The present invention relates to a process for the preparation of a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein R represents one or more groups independently selected from fluorine, chlorine, bromine, and iodine, said process comprising the cyclopropanation of a compound of formula (II) with ethylene carbonate or ethylene sulfate: wherein X is chlorine, bromine, iodine or a triflate group (CF3SO3) or a group wherein R is as defined above and G is —CN or —COOR2 wherein R2 is a C1-C4 straight or branched alkyl chain.

Abstract: The present invention relates to a process for preparing Nebivolol and, more in particular, to a fractional distillation method of a mixture of stereoisomers of formula intermediates useful in the preparation of nebivolol.

Abstract: The present invention relates to a process for preparing Bosentan Monohydrate; in particular, the present invention provides the preparation of the novel 4-tert-butyl-N-[6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-2-(2-pyrimidinyl)-pyrimidin-4-yl]-benzenesulfonamide sodium salt as an ethylene glycol solvate (Bosentan sodium salt ethylene glycol solvate), which is a useful intermediate for obtaining Bosentan Monohydrate in a pure form.

Abstract: The present invention relates to a process for preparing Nebivolol and, more particularly, to an improved method of debenzylation of a compound of formula (II) useful for preparing nebivolol endowed with high purity.

Abstract: The present invention relates to a process for the preparation of a compound of formula (I) or a pharmaceutically acceptable salt thereof: wherein R represents one or more groups independently selected from fluorine, chlorine, bromine, and iodine, said process comprising the cyclopropanation of a compound of formula (II) with ethylene carbonate or ethylene sulfate: wherein X is chlorine, bromine, iodine or a triflate group (CF3SO3) or a group ?wherein R is as defined above and G is —CN or —COOR2 wherein R2 is a C1-C4 straight or branched alkyl chain.

Abstract: The present invention relates to a process for preparing Bosentan Monohydrate; in particular, the present invention provides the preparation of the novel 4-tert-butyl-N-[6-(2-hydroxy-ethoxy)-5-(2-methoxy-phenoxy)-2-(2-pyrimidinyl)-pyrimidin-4-yl]-benzenesulfonamide sodium salt as an ethylene glycol solvate (Bosentan sodium salt ethylene glycol solvate), which is a useful intermediate for obtaining Bosentan Monohydrate in a pure form.

Abstract: The present invention relates to a process for preparing nebivolol and, more particularly, to a process for preparing d-nebivolol and its enantiomer l-nebivolol or acid addition salts thereof starting from commercially available or easily obtainable 2,2-dimethyl-1,3 dioxolane-4-carbaldehyde and a vinyl Grignard reagent.

Abstract: A process for resolving dorzolamide trans racemate, which comprises reacting said racemate with (1S)-(+)-10-camphorsulfonic acid so obtaining the (4S,6S) enantiomer by selectively precipitating and recovering the camphorsulfonic acid salt thereof (dorzolamide camphorsulfonate), and neutralizing dorzolamide camphorsulfonate to obtain dorzolamide.

Abstract: The present invention relates to a process for preparing Nebivolol and, more in particular, to a fractional distillation method of a mixture of stereoisomers of formula intermediates useful in the preparation of nebivolol.

Abstract: The present invention relates to a process for reducing a compound of formula (I) wherein X is halogen, a hydroxy group, an alkylsulfoniloxy group or an arylsulfonyloxy group; to give a compound of formula (II) as a diastereoisomerically pure compound of RS/SR configuration characterized in that said reduction is carried out by the use of (+)-B-chlorodiisopinocampheylborane or (?)-B-chlorodiisopinocampheylborane. The compounds of formula (II) are useful as intermediates for the preparation of Nebivolol.

Abstract: The present invention relates to a process for preparing Nebivolol and, more particularly, to an improved method of debenzylation of a compound of formula (II) useful for preparing nebivolol endowed with high purity.

Abstract: The present invention relates to a process for preparing Nebivolol and, more particularly, to an improved process for synthesizing enantiomerically enriched 6-fluoro chroman alcohol or epoxide derivatives of formula, wherein R and X is defined in the description; as useful intermediates in the preparation of Nebivolol.

Abstract: The present invention relates to a process for preparing nebivolol and, more particularly, to a process for preparing d-nebivolol and its enantiomer l-nebivolol or acid addition salts thereof starting from commercially available or easily obtainable 2,2-dimethyl-1,3 dioxolane-4-carbaldehyde and a vinyl Grignard reagent.

Abstract: The present invention relates to a process for preparing nebivolol and, more particularly, to a process for preparing d-nebivolol and its enantiomer l-nebivolol or acid addition salts thereof starting from commercially available or easily obtainable 2,2-dimethyl-1,3 dioxolane-4-carbaldehyde and a vinyl Grignard reagent.

Abstract: The present invention relates to a process for the preparation of Nebivolol and, more particularly, to an improved method of synthesizing 6-fluoro chroman epoxides of formula (I) key intermediates in preparing nebivolol.

Abstract: The present invention relates to macrolide compounds endowed with antiinflammatory activity and more particularly relates to new stable crystalline forms of a macrolide derivative with antiinflammatory activity, processes for the preparation of such forms, pharmaceutical compositions containing them as active ingredient and the use of said crystalline forms for the treatment of inflammatory diseases.