Abstract: A new process is disclosed for the synthesis of fluconazole monohydrate and for crystal modifications of fluconazole which comprises the step of hydrolyzing a silyl ether of the formula (II) ?wherein R2 is hydrogen, or a C1 to C10 alkyl or phenyl group, R3 and R4 independently of each other are a C1 to C10 alkyl or phenyl group in an aqueous solution, preferably at a pH below 3 or above 8.

Abstract: A new process is disclosed for the synthesis of fluconazole monohydrate and for crystal modifications of fluconazole which comprises the step of hydrolyzing a silyl ether of the formula (II) 1

Abstract: A Process is disclosed for preparing a compound of the Formula (I) which comprises the steps of: (a) detritylating a compound of the Formula (III)  with 0.1 to 1 equivalent of potassium hydroxide in a C1 to C4 straight chain alcohol solvent to obtain a reaction mixture containing the compound of the Formula (I), (b) changing the C1 to C4 straight chain alcohol solvent in the reaction mixture to an aprotic solvent or a weakly protic solvent, and (c) following step (b) crystallizing out the compound of the Formula (I) from the reaction mixture.

Abstract: A process is disclosed for the preparation of compounds of the formula (I), which compounds are useful as intermediates for the preparation of paroxetine of formula(V).

Abstract: The invention relates to a process for the synthesis of losartan potassium of formula (I), chemical name: 2-n-butyl-4-chloro-1-[(2′-(tetrazol-5-yl)-1,1′biphenyl-4-yl)-methyl]-imidazol-5-methanol potassium, starting from 2-n-butyl-4-chloro-1-[(2′-(2-triphenylmetyl-2H-tetrazol-5-yl)-1,1′-biphenyl-4-yl)-methyl]-1H-imidazol-4-methanol of formula (III). According to the process the compound of formula (III) is reacted in an alcohol of formula (VI),—wherein the meaning of R is C1-C4 straight chain alkyl group—with 0.1-1 equivalent of potassium hydroxide. The final product of formula (I) is isolated after crystallizing out by changing the solvent to an aprotic or weakly protic solvent (I).

Abstract: The invention relates to novel racemic and optically active trans apovincaminic acid ester derivatives of formula (I), ##STR1## wherein R means hydrogen or a group (a), wherein Z stands for C.sub.1-4 alkyl, optionally substituted aryl, aralkyl, heteroaryl or 14-eburnameninyl group; and n is an integer of 2, 3 or 4, as well as therapeutically acceptable salts thereof. The invention further relates to pharmaceutical compositions containing these compounds as well as a process for the preparation of the above compounds and compositions, and in addition, to a method of treatment. The novel compounds of Formula (I) exhibit particularly antioxidant, antiischemic as well as antiamnesic effects and are useful for inhibiting lipid peroxidation and for protection from or treatment of ischemia and amnesia as well as for treating various degenerative neurological diseases, e.g. Alzheimer's disease.

Abstract: Anti-Fungal compounds are disclosed of the Formula (I) ##STR1## wherein R.sup.1 is C.sub.1 to C.sub.10 alkyl, phenyl, or phenyl-C.sub.1 to C.sub.6 alkyl, and the phenyl moiety of the two latter groups may carry at least one substituent selected from the group consisting of a halogen atom,C.sub.1 to C.sub.6 alkoxy group, phenyl group, phenoxy group, and trifluorome thyl group;R.sup.2 is a hydrogen atom, a C.sub.1 to C.sub.10 alkyl group or a phenyl group;R.sup.3 and R.sup.4 are independently from each other a C.sub.1 to C.sub.10 alkyl group or a phenyl group;X is a hydrogen atom, halogen atom or a group of the formula (A) ##STR2## and in this formula Y.sup.1 and Y.sup.2 are independently from each other, a --N.dbd. atom or a group of the formula --CH.dbd., or an optical antipode thereof.

Abstract: The invention relates to a novel process for the preparation of (-) -1.beta.-ethyl-1.alpha.-(hydroxymethyl) - 1,2,3,4,6,7,12,12b.alpha.-octahydro-indolo[2,3-a]quinolizine of the formula (I) ##STR1## and to novel intermediates obtained in this process. The compound of the formula (I) prepared by the process of the invention possesses a peripheral vasodilator effect.

Abstract: A method of treating a mammalian subject for Parkinson's disease or to provide a central muscle relaxant effect, which comprises the step of administering to the mammalian subject in need of the treatment, a therapeutically effective amount of a compound of the Formula (I) ##STR1## wherein m is 1,2 or 3;R.sub.1 and R.sub.2 each independently stand for hydrogen, C.sub.1 to C.sub.4 straight or branched chain alkyl, C.sub.1 to C.sub.4 alkoxy, C.sub.5 to C.sub.7 cycloalkyl, or halogen; andB is a 5- or 6-membered saturated or unsaturated heterocyclic group containing a nitrogen heteroatom, the heterocyclic group being bound through its heterocyclic nitrogen atom to the remainder of the compound, and which can contain one or two additional heteroatoms selected from the group consisting of an oxygen heteroatom, a sulfur heteroatom, and one or two additional nitrogen heteroatoms, which may be as an .dbd.N--, --NH-- or --NR-- group, where R is a C.sub.1 to C.sub.5 alkyl or C.sub.1 to C.sub.

Abstract: The present invention relates to racemic or optically active cis octahydro-indolo [2,3-a] quinolizine diester derivatives.

Abstract: A method of treating a mammalian subject for Parkinson's disease or to provide a central muscle relaxant effect, which comprises the step of administering to the mammalian subject in need of the treatment, a therapeutically effective amount of a compound of the Formula (I) ##STR1## wherein m is 1,2 or 3;R.sub.1 and R.sub.2 each independently stand for hydrogen, C.sub.1 to C.sub.4 straight or branched chain alkyl, C.sub.1 to C.sub.4 alkoxy, C.sub.5 to C.sub.7 cycloalkyl, or halogen; andB is a 5- or 6-membered saturated or unsaturated heterocyclic group containing a nitrogen heteroatom, the heterocyclic group being bound through its heterocyclic nitrogen atom to the remainder of the compound, and which can contain one or two additional heteroatoms selected form the group consisting of an oxygen heteroatom, a sulfur heteroatom, and one or two additional nitrogen heteroatoms, which may be as an .dbd.N--, --NH-- or --NR-- group, where R is a C.sub.1 to C.sub.5 alkyl or C.sub.1 to C.sub.

Abstract: New intermediate compounds are disclosed of the formula I, ##STR1## wherein R.sub.1 and R.sub.2 are independently alkyl having 1 to 4 carbon atoms,or acid-addition salts thereof of formula Ib, ##STR2## wherein X represents an acid residue, and a process for the preparation of the intermediate compounds.

Abstract: An antifungal or anthelmintic method of treatment is disclosed which comprises the step of administering to a mammal in need of said treatment, a pharmaceutically effective amount of a compound of the Formula (I) ##STR1## wherein X is halogen, C.sub.1 to C.sub.6 alkoxy, or a group --NRR.sup.1 in which R and R.sup.1 are each hydrogen or C.sub.1 to C.sub.6 alkyl; andR.sup.2 is hydrogen, halogen, C.sub.1 to C.sub.6 alkyl, C.sub.1 to C.sub.6 alkoxy, phenyl, phenylthio, or phenyl or phenylthio substituted by at least one halogen or amino substituent; or a pharmaceutically acceptable acid addition salt thereof.

Abstract: The invention relates to a new process for preparing 6-amino-1,2-dihydro-1-hydroxy-2-imino-4-piperidinopyrimidine of the formula (I), ##STR1## which comprises reacting a pyrimidine derivative of the general formula (II), ##STR2## wherein R.sub.1 stantds for hydrogen or a ##STR3## group, wherein R means a C.sub.1-6 alkyl group or an aryl group optionally substituted by halogen;R.sub.2 stands for a hydroxyl group or an ##STR4## group, wherein R is as defined above; andX represents chlorine or bromine or an optionally mono- or polysubstituted arenesulfonyloxy group,with the proviso that R.sub.2 is different from a hydroxyl group when R.sub.1 stands for hydrogen, with piperidine and hydrolyzing, optionally after isolation, the thus-obtained 4-piperidino derivative of the general formula (III), ##STR5## wherein R.sub.1 and R.sub.2 are as defined above.

Abstract: The invention relates to a new process for the preparation of nitraminodiaryl sulfoxide derivatives of the formula (I), ##STR1## wherein R and R.sup.1 represent hydrogen or alkyl having from 1 to 6 carbon atoms, andR.sup.2 is hydrogen, halogen, alkyl having from 1 to 6 carbon atoms, alkoxy having from 1 to 6 carbon atoms, or phenyl or thiophenyl both optionally substituted by one or more identical or different halogen(s) and/or nitro group(s).The compounds of formula (I) are pharmaceutically active, and are particularly useful in the veterinary therapy as anthelmintics. In addition they show pesticidal, particularly acaricidal, fungicidal and herbicidal properties. The invention relates also to pharmaceutical and pesticidal compositions containing as active ingredient compounds of formula (I).The compounds of formula (I), in which the substituents are as defined, with the proviso that if R.sup.2 is hydrogen and the substituent --N(R,R.sup.1) is in para-position related to the sulfoxide group, R and R.sup.

Abstract: The invention relates to the preparation of cis and trans stereoisomers of racemic and optically active eburnamenine derivatives of the general formula (Ia) ##STR1## or (Ib), ##STR2## wherein R.sub.1 stands for a C.sub.1-4 alkyl group; andR stands for hydrogen, a C.sub.1-6 alkyl group, a C.sub.2-6 alkenyl group, an acyl or substituted acyl group,as well as their acid addition salts, of which the trans compounds are novel.The invention also relates to the compounds of the general formula (IIIa) ##STR3## and (IIIb), ##STR4## wherein R.sub.1 and R' represent a C.sub.1-4 alkyl group. The compounds of the general formulae (Ia) and (Ib) possess a vasodilatory effect which is substantially higher than that of pentoxifyllin, a known peripheral vasodilator.

Abstract: The invention relates to a new process for the preparation of aminodiaryl sulfoxide derivatives of the formula (I), ##STR1## wherein X is halogen, alkoxy having from 1 to 6 carbon atoms or a group --(N,R,R.sup.1), in which p1 R and R.sup.1 are hydrogen or alkyl having from 1 to 6 carbon atoms,R.sup.2 is hydrogen, halogen, alkyl having from 1 to 6 carbon atoms, alkoxy having from 1 to 6 carbon atoms or phenyl or phenylthio both optionally substituted by one or more identical or different halogen(s) and/or amino group(s),and acid addition salts thereof.The compounds of formula (I) are pharmaceutically active, in particular are potent anthelmintics, or can be used as active ingredients in pesticidal compositions. The invention therefore relates to pharmaceutical and pesticidal compositions containing compounds of formula (I) or salts thereof as active ingredient.Compounds of formula (I), in which the substituents are as defined above, but if X stands for a group --N(R,R.sup.1) in which R and R.sup.

Abstract: A pyrimidine derivative of the formulae (Ia), (Ib) and (Ic), ##STR1## wherein R stands for an alkyl group group with 1 to 6 carbon atoms or an aryl group optionally substituted by halogen atom; andX stands for chlorine or bromine atom or an arylsulfonyloxy group optionally substituted by 1 to 3 lower alkyl groups.The subject pyrimidine derivatives are intermediates for preparing 6-amino-1,2-dihydro-1-hydroxy-2-imino-4-piperidinopyrimidine.

Abstract: The invention relates to new eburnane derivatives of the formula (I) ##STR1## wherein R.sup.1 is alkyl having from 1 to 6 carbon atoms, and acid addition salts thereof.The invention further relates to a process for the preparation of these compounds and pharmaceutical compositions containing them.Compounds of formula (I) show remarkable CNS-activity and are useful intermediates in the preparation of other, pharmaceutically active compounds.

Abstract: The invention relates to a new process for the preparation of aminodiaryl sulfoxide derivatives of the formula (I), ##STR1## wherein X is halogen, alkoxy having from 1 to 6 carbon atoms or a group --(N,R,R.sup.1), in whichR and R.sup.1 are hydrogen or alkyl having from 1 to 6 carbon atoms,R.sup.2 is hydrogen, halogen, alkyl having from 1 to 6 carbon atoms, alkoxy having from 1 to 6 carbon atoms or phenyl or phenylthio both optionally substituted by one or more identical or different halogen(s) and/or amino group(s),and acid addition salts thereof.The compounds of formula (I) are pharmaceutically active, in particular are potent anthelmintics, or can be used as active ingredients in pesticidal compositions. The invention therefore relates to pharmaceutical and pesticidal compositions containing compounds of formula (I) or salts thereof as active ingredient.Compounds of formula (I), in which the substituents are as defined above, but if X stands for a group --N(R,R.sup.1) in which R and R.sup.