Abstract: The present invention relates to a method for preparation of the tetrasaccharide lacto-N-neotetraose (LNnt, formula (I)) especially in large scale, as well as intermediates in the synthesis, a new crystal form (polymorph) of LNnt, and the use thereof in pharmaceutical or nutritional compositions.

Abstract: The present invention relates to novel polymorphs of the trisaccharide 2?-O-fucosyllactose (2-FL) of formula (1), methods for producing said polymorphs and their use in pharmaceutical or nutritional compositions.

Abstract: A method for purifying, separating and/or isolating an oligosaccharide or a salt thereof is presented. An embodiment of the invention is based upon the formation of anomeric O-benzyl/substituted O-benzyl derivatives in a selective anomeric alkylation reaction.

Abstract: The present invention relates to novel polymorphs of the trisaccharide 2?-O-fucosyllactose (2-FL) of formula (1), methods for producing said polymorphs and their use in pharmaceutical or nutritional compositions.

Abstract: The present invention relates to a method for preparation of the tetrasaccharide lacto-N-neotetraose (LNnt, formula (I)) especially in large scale, as well as intermediates in the synthesis, a new crystal form (polymorph) of LNnt, and the use thereof in pharmaceutical or nutritional compositions.

Abstract: According to the present invention, 2-chloroethoxy-acetic acid-N,N-dimethylamide of the Formula (I) is prepared by reacting 2-hydroxyethoxy-acetic acid-N,N-dimethylamide of the Formula (II) in a solvent optionally in the presence of a catalyst with thionyl chloride and removing the solvent by distillation.

Abstract: The present invention is related to 1-[(4-chlorophenyl)-phenylmethyl]-4-(2,2,2-trichloroethoxycarbonyl)-piperazine of the Formula (IV) and optically isomers thereof, process for preparation thereof and the use of the compound of the Formula (IV) in the preparation of 1-(4-chlorophenyl)-phenylmethyl-piperazine and optical isomers and salts thereof. 1-(4-chlorophenyl)-phenylmethyl-piperazine and optical isomers thereof are important intermediates in the preparation of non-sedating antihistamine-type active pharmaceutical ingredients.

Abstract: According to the present invention, 2-chloroethoxy-acetic acid-N,N-dimethylamide of the Formula (I) is prepared by reacting 2-hydroxyethoxy-acetic acid-N,N-dimethylamide of the Formula (II) in a solvent optionally in the presence of a catalyst with thionyl chloride and removing the solvent by distillation.

Abstract: The present invention is related to 1-[(4-chlorophenyl)-phenylmethyl]-4-(2,2,2-trichloroethoxycarbonyl)-piperazine of the Formula (IV) and optically isomers thereof, process for preparation thereof and the use of the compound of the Formula (IV) in the preparation of 1-(4-chlorophenyl)-phenylmethyl-piperazine and optical isomers and salts thereof. 1-(4-chlorophenyl)-phenylmethyl-piperazine and optical isomers thereof are important intermediates in the preparation of non-sedating antihistamine-type active pharmaceutical ingredients.

Abstract: The present invention relates to a process for the preparation of {2-[4-(?-phenyl-p-chlorobenzyl)-piperazin-1-yl]-ethoxy}-acetic acid-N,N-dimethylamide of the Formula (I) and enantiomers thereof. The compound of the Formula (I) or enantiomers thereof are important pharmaceutical intermediates suitable for direct transformation into non-sedating antihistamine type pharmaceutical active ingredients cetirizine and levocetirizine.

Abstract: The invention refers to a novel process for the preparation of {2-[-(?-phenyl-p-chlorobenzyl)piperazin-1-yl]ethoxy}acetic acid, which comprises hydrolyzing an N,N-disubstituted {2-[-(?-phenyl-p-chlorobenzyl)piperazin-1-yl]ethoxy}acetamide, wherein said substituents are selected from alkyl groups having 1 to 4 carbon atoms optionally substituted by a phenyl group, alkenyl groups having 2 to 4 carbon atoms or cyclohexyl groups, or the substituents together with the adjacent nitrogen atom of the acetoamido group, form a morpholino group.

Abstract: The invention refers to a novel process for the preparation of cetirizine of formula (I) as well as to novel {2-[4-(&agr;-phenyl-p-chloro-benzyl)piperazin-1-yl]ethoxy}acetamides of formula II, wherein R1 and R2 represent, independently, a C1-4 alkyl group optionally substituted by a phenyl group, a C2-4 alkenyl group or a cyclohexyl group, or R1 and R2 form together with the adjacent nitrogen atom a morpholino group. According to the novel process, an acetamide of formula (II) is hydrolized, if desired in the presence of a phase transfer catalyst, to obtain cetirizine.

Abstract: The invention refers to novel 2-(1,2,4-triazole-1-yl)-1,3,4-thiadiazole derivatives of formula (I) having an influence on the heart and the central nervous system, furthermore pharmaceutical compositions containing the above derivatives, and a process for the preparations of the novel compounds.

Abstract: This invention relates to a new and improved process for the preparation of 6,7-dichloro-1,5-dihydroimidazo[2,1-b]-quinazolin-2[3H]-one of formula ##STR1## (anagrelide), a valuable blood platelet antiaggregative compound. According to the process of the invention the compound of formula (I) is prepared by subjecting a new 2-cyanoiminoquinazoline derivative of the general formula ##STR2## wherein R stands for cyano or a group of the formula COOR.sup.1, in the latter R.sup.1 representing lower alkyl optionally carrying a phenyl substituent, to thermal cyclization in an acidic medium.The invention also relates to new 2-cyanoiminoquinazo-lines of the general formula (III) used for the production of anagrelide and to the preparation of the said compounds.The invention provides an advantageous process for the preparation of anagrelide which is devoid of the drawbacks of the hitherto known processes and renders possible the production of the compound of the formula (I) on industrial scale, too.

Abstract: This invention relates to novel triazolopyrimidine derivatives of formulae (Ia) and (Ib), ##STR1## wherein Q represents hydrogen, a heterocyclic group optionally substituted by a C.sub.1-4 alkyl group and containing one or more oxygen and/or nitrogen atoms or a group of formula--SR.sup.1 wherein R.sup.1 is alkyl or aralkyl, or a group of formula--NR.sup.2 R.sup.3 wherein R.sup.2 and R.sup.3 are independently hydrogen, alkyl, alkenyl, cycloalkyl, aralkyl, aryl or a heterocyclic group,m and n are independently 0, 1, 2, 3 or 4, with the provision that if m stands for 0, then n is different from 0, and if both n and m are 1 or m stands for 0 and n is 2, the Q is different from methylthio or morpholino group, their mixtures or pharmaceutically acceptable salts. Furthermore, the invention relates to a process for preparing these compounds.The compounds of formulae (Ia) and (Ib) are able to inhibit the ptosis caused by tetrabenazine and they have analgetic activity.