PROCESS FOR PREPARING 2- AND 4- ALKOXYCARBONYL THIOLAN-3-ONES

Heterocyclic compounds

Pyridine derivatives, which are intermediates in the production of pharmaceutically active compounds, have the formula <IMAGE> wherein R<1> and R<2> each independently represent hydrogen, lower alkyl, lower alkoxy, carboxyloweralkyl, carboxy, hydroxyloweralkyl, halogen, haloloweralkyl, lower alkoxycarbonyl, optionally substituted aryl or optionally substituted aralkyl, n represents an integer from 3 to 6; R<3> represents hydrogen or single or multiple substitution on one or more of the aliphatic carbons by one or more substituents selected from lower alkyl, optionally substituted aryl and optionally substituted aralkyl; R<5> and R<7> each independently represent hydrogen or lower alkyl; p is 0 or 1; P<1> and P<2> each represent an optional organic silyl protecting group on the carbon in the epi position to the nitrogen; and M is Na, K, Li or MgHal in which Hal is a halogen atom.

PYRROLIDINES, PIPERIDONES AND HEXAHYDROAZEPINONES

META HYDROXYPHENYL SUBSTITUTING CONNECTIONS.

VERFARHEN FOR THE PRODUCTION OF ALPHA ARYL GAMMA BUTYROLACTONEN

AZETIDINCARBOXAMIDDERIVATE FOR THE TREATMENT OF ZNS ILLNESSES

AZETIDINCARBOXAMIDDERIVATE FOR THE TREATMENT OF ZNS ILLNESSES

NOVEL PROCESSES AND INTERMEDIATES FOR THE PREPARATION OF PIPERAZINE DERIVATIVES

Compounds having the formula R5O-A-NR4-R2 (V), where R2 is a heteroaryl grou p linked to the remainder of the molecule via a carbon atom adjacent a nitrogen atom and R4 and R5 are both hydrogen atoms o r together represent -SO- or -SO2- and A is C2-C4 alkylene optionally substituted by one or more lower alkyl groups are novel intermediates in the preparation of pharmaceutically useful piperazine derivatives as end compounds. The compounds having formula (V) where R4 and R5 are hydrogen may be prepared by a rearrangement of a compound having the formula R2-O-A-NH2 (VI).

Verfahren zur Herstellung von 2-und 4-alkoxycarbonyl Thiolan-3-onen.

SUBSTITUTED 1,3- DIAMINOPROPANES

N min -Acyl-N-alkyl-1,3-diaminopropanes of formula R<1>CONH(CH2)3NHR<2> (where R<1> is R- or RNH where R is a substituted or unsubstituted hydrocarbon group and R<2> is alkyl) are prepared by selectively acylating N-alkyl-1,3-diaminopropanes. In the process a N-alkyl-1,3-aminopropane is reacted with an aldehyde to form a hexahydropyrimidine, the hexahydropyrimidine is acylated and the acylated hexahydropyrimidine is then hydrolysed to give the product.

PREPARATION OF CYCLOHEXANOL DERIVATIVES AND NOVEL THIOAMIDE INTERMEDIATES

PIPERIDINE DERIVATIVES

PREOCESS FOR PREPARING PYRIDINE DERIVATIVES

VERFARHEN ZUR HERSTELLUNG VON ALPHA-ARYL-GAMMA-BUTYROLACTONEN

PCT No. PCT/GB93/02427 Sec. 371 Date May 16, 1995 Sec. 102(e) Date May 16, 1995 PCT Filed Nov. 25, 1993 PCT Pub. No. WO94/12487 PCT Pub. Date Jun. 9, 1994This appliciation discloses a process for preparing a lactone of general formula (I), where R is an optionally substituted phenyl group or an optionally substituted mono- or bicyclic heteroaryl radical which process comprises reacting an anion of a malonate of formula (II) with an ethylene compound of formula (III) Y-CH2-CH2OZ, to give a compound of formula (IV) and hydrolysing the compound of formula (IV) to give a lactone of formula (I). The lactones are of use as intermediates for preparing 5-HT1A binding agents. <IMAGE> (I) <IMAGE> (II) <IMAGE> (IV)

PYRIDINDERIVATE, VERFAHREN ZUR HERSTELLUNG UND ARZNEIMITTEL

CYCLOHEXANOL DERIVATIVES.

Compounds having the formula I where R<1> is -CN, -CO-N(CH3)2 or -CS-N(CH3)2 and R<2> is hydrogen, methyl or a removable protecting group are prepared by condensing a compound having the formula where M is lithium, sodium, potassium or halomagnesium and R<3> is methyl or a removable protecting group, with cyclohexanone in a solvent comprising 80-100% of one or more hydrocarbons and 0-20% of one or more ethers. The solvent enables less inconvenient reaction temperatures to be used and higher yields to be obtained. Compounds (I) are new per se where R<1> is -CS-N(CH3)2. Compounds (I) are chemical intermediates for preparing N, N-dimethyl-2-(1-hydroxycyclohexyl)-2-(4-hydroxyphenyl or 4-methoxyphenyl) ethylamine and pharmaceutically acceptable salts thereof. These end products are antidepressants.

METHOD OF PREPARING 2-OXO- AND 2-UNSUBSTITUTED-HEXAHYDROAZEPINE DERIVATIVES

Preparation of 3-Alkoxycycloalk-2-en-1-ones

Compounds of formula (I> wherein n is 1 or 2, X is hydrogen, C1-6 alkyl, chlorine or bromine, R<2> is C1-6 alkyl and R and R<1> each represent H, C1-6 alkyl, aryl, arylalkyl or C1-6 alkoxy, are prepared by reacting a compound of formula (II> with a C1-6 alkyl orthoformate in an alcohol solvent in presence of a catalytic amount of an acid ion exchange resin.

PROCESS FOR PREPARING THIAZOLOBENZIMIDAZOLES AND INTERMEDIATES USED THEREIN

M-HYDROXYPHENYL SUBSTITUTED COMPOUNDS

Oxathiazolidinyl pyridines

Compounds having the formulawhere R2 is a heteroaryl group linked to the remainder of the molecule via a carbon atom adjacent a nitrogen atom and R4 and R5 are both hydrogen atoms or together represent -SO- or -SO2- and A is C2-C4 alkylene optionally substituted by one or more lower alkyl groups are novel intermediates in the preparation of pharmaceutically useful piperazine derivatives as end compounds. The compounds having formula V where R4 and R5 are hydrogen may be prepared by a rearrangement of a compound having the formula (VI).

Process for preparing 2-and 4-alkoxycarbonylthiolan-3-ones

The invention concerns a process for preparing 2- and 4-alkoxycarbonylthiolan-3-ones useful as intermediates, which process involves cyclising a 3-akloxycarbonylmethylthiopropanoic acid ester using lithium alkoxide. Novel lithium salts are also included.

PROCESS FOR THE PREPARATION OF ALPHA-ARYL-GAMMA-BUTYROLACTONES

A process for preparing a lactone of general formula (I), where R is an optionally substituted phenyl group or an optionally substituted mono- or bicyclic heteroaryl radical which process comprises reacting an anion of a malonate of formula (II) with an ethylene compound of formula (III) Y-CH2-CH2OZ, to give a compound of formula (IV) and hydrolysing the compound of formula (IV) to give a lactone of formula (I). The lactones are of use as intermediates for preparing 5-HT1A binding agents.

2-arycalicyl-pyridine derivatives

The invention concerns compounds of formula I (I) or a salt thereof, wherein R1 and R2 each independently represent hydrogen, lower alkyl, lower alkoxy, carboxyloweralkyl, carboxy, hydroxyloweralkyl, halogen, haloloweralkyl, lower alkoxycarbonyl, optionally substituted aryl or optionally substituted aralkyl, n represents an integer from 3 to 6; R3 represents hydrogen or single or multiple substitution on one or more of the aliphatic carbons by one or more substituents selected from lower alkyl, optionally substituted aryl and optionally substituted aralkyl; A represents a group of formula (i) or (ii) below: -CR4R5-(CR6R7)m-(i) -CX-(CR6R7)m-(ii) in which R4, R6 and R7 each independently represent hydrogen or lower alkyl (providing that when R5 is NH2, R4 is hydrogen); m is O or 1; R5 represents hydrogen, NH2, OH or loweralkoxy, and X is =O, =NH or =NOH, the attachment of A to B being from either end, and B represents a optionally substituted aryl or heteroaryl radical which compounds possess ...

Piperidine derivatives

Piperidine derivatives of formula and esters thereof, and pharmaceutically acceptable acid addition salts of the alcohols or esters, wherein R<2> is a phenyl group optionally substituted by one or more specified substituents and R<6> is hydrogen, aryl(lower)alkyl or cycloalkyl(lower)alkyl possess pharmacological activity (e.g. as analgesics, antidepressants or anti-secretary agents) or are intermediates for compounds possessing such activity.

M-HYDROXYPHENYL SUBSTITUTED COMPOUNDS

THIENO2,3-A QUINOLIZIN-9-YL SULPHONAMIDES

The invention concerns thienoquinolizines of general formula (I) (I) and their pharmaceutically acceptable acid addition salts. In the formula R1 is hydrogen or lower alkyl and R2 is lower alkyl, halo(lower)alkyl, -A-NR3R4 ?where A represents a direct bond between the S and N atoms or a lower alkylene group having 1 to 3 carbon atoms in the chain between the S and N atoms and R3 and R4 each independently represent hydrogen, lower alkyl, aryl or aryl(lower)alkyl or together with the nitrogen atom to which they are attached represent a five or six membered heterocyclic ring!, aryl or a heterocyclic radical or R1 is -A1NR5.SO2R6 ?where A1 is a lower alkylene group having 1 to 3 carbon atoms in the chain between the two N atoms, R5 is hydrogen or lower alkyl and R6 is lower alkyl, halo(lower)alkyl or aryl! and R2 is lower alkyl, halo(lower)alkyl or aryl. The compounds possess alpha 2-adrenoceptor antagonistic activity in warm blooded animals.

PROCESS FOR PREPARING THIAZOLOBENZIMIDAZOLES AND INTERMEDIATES USED THEREIN

PROCESS FOR PREPARING PYRIDINE DERIVATIVES

Preparation of tetrahydroquinolines and related compounds

An improved process for preparing tetrahydroquinolines and related compounds especially 5,6,7,8-tetrahydroquinoline-8-nitriles, amides and thioamides is described. The nitriles and thioamides are anti-ulcer and/or anti-secretory agents. Typically a compound of formula A A where M is sodium, potassium, lithium or MgHal where Hal is chlorine, bromine or iodine, is reacted, e.g., in an ether solvent, with a silyl compound RxaSi(NCY)4-x(III) wherein Ra is alkyl, cycloalkyl, aralkyl, or aryl, at least one group Ra being a branched chain alkyl, cycloalkyl, aryl or branched chain aralkyl, Y is oxygen or sulphur, x has a value from 1 to 3, then subjecting the product to hydrolysis or alcoholysis, to obtain the corresponding nitrile, amide or thioamide, provided that when a nitrile is desired the molar ratio of compound III to compound A is at least 2:1 and x is 3 and Y is S. The products may be obtained as acid addition salts. Compound A may contain various substituents, e.g., hydrocarbon substituents ...

Preparation of nitriles and thioamides of fused ring pyridine derivatives

Nitriles and thiomides of fused ring pyridine compounds such as 5,6,7,8-tetrahydroquinolines are prepared from metal derivatives of the starting compounds (such as 8-lithio- 5,6,7,8-tetrahydroquinolines) which have been prepared by treating the starting compounds (e.g. 5,6,7,8- tetrahydroquinoline) with a metal amide prepared in situ from a metal alkyl and an N-benzylidine-N- alkylamine.

m-Hydroxypheny1 substituted compounds

... m-Hydroxyphenyl substituted compounds of formula where R is an organic radical and R<1> is hydrogen or an organic radical are prepared by dehydrohalogenating a compound of formula (where X is chlorine or bromine, and R and R<1> have the above meanings). Preferred novel starting materials of formula (II) are of the formula (where R<1> and X are as above, n is 2, 3 or 4, R<2> is hydrogen or lower alkyl and R<3> is hydrogen, lower alkyl, lower alkenyl, lower alkynyl, cycloalkyl(lower)alkyl or aryl(lower)alkyl).

Process for preparing bromo-pyridine derivatives

Compounds of formula wherein R<1> and R2 each independently represent hydrogen, lower alkyl, lower alkoxy, carboxyloweralkyl, carboxy, hydroxyloweralkyl, halogen, haloloweralkyl, lower alkoxycarbonyl, optionally substituted aryl or optionally substituted aralkyl, n represents an integer from 3 to 6; R<3> represents hydrogen or single or multiple substitution on one or more of the aliphatic carbons by one or more substituents selected from lower alkyl, optionally substituted aryl and optionally substituted aralkyl, are prepared by reacting a compound of formula with either HBr and bromine or with bromine in an inert solvent.

NOVEL SILYL REAGENTS AND THEIR PREPARATION

THIENO2,3-A QUINOLIZIN-9-YL SULPHONAMIDES

Process for preparing benzimidazoles and intermediates used therein

The invention concerns a process for preparing a thiazolo?3,2-a!benzimidazole of formula I in which formula n is 1 or 2, and R1 is hydrogen, lower alkyl, lower alkoxy, trifluoromethyl or halo, or a salt thereof which comprises dehydrating a compound of formula II, or a salt thereof wherein n and R, are as defined above, and COOR is an acid or ester function in the presence of an acid selected from sulphuric, sulphonic and phosphoric acid or mixtures thereof and if desired or required an inert solvent provided that if water is present then the amount of water is less than about 15% by volume of the acid, the reaction being carried out with heating if necessary.

NOVEL SILYL DERIVATIVES

PREPARATION OF TETRAHYDROQUINOLINES AND RELATED COMPOUNDS

PREPARATION OF 3-ALKOXYCYCLOALK-2-EN-1-ONES

PREOCESS FOR PREPARING PYRIDINE DERIVATIVES

PROCESS FOR PREPARING THIAZOLOBENZIMIDAZOLES AND INTERMEDIATES USED THEREIN

Process for the preparation of alpha-aryl-gamma-butyrolactones

Processes and intermediates for the preparation of piperazine derivatives

Compounds having the formulawhere R2 is a heteroaryl group linked to the remainder of the molecule via a carbon atom adjacent a nitrogen atom and R4 and R5 are both hydrogen atoms or together represent -SO- or -SO2- and A is C2-C4 alkylene optionally substituted by one or more lower alkyl groups are novel intermediates in the preparation of pharmaceutically useful piperazine derivatives as end compounds. The compounds having formula V where R4 and R5 are hydrogen may be prepared by a rearrangement of a compound having the formula (VI).

HEXAHYDROAZEPINE, PIPERIDINE AND PYRROLIDINE DERIVATIVES AND PROCESSES FOR MAKING AND USING THEM

M-HYDROXYPHENYL SUBSTITUTED COMPOUNDS

Verfahren zur Herstellung von 2-und 4-alkoxycarbonyl Thiolan-3-onen.

VERFAHREN ZUR HERSTELLUNG VON THIAZOLOBENZIMIDAZOLEN UND ZWISCHENPRODUKTE.

Azetidinecarboxamide derivatives for treating CNS disorders

A compound of formula (1) wherein R<1 >is aryl; and R<2 >is hydrogen or alkyl; pharmaceutically acceptable addition compounds thereof; and their use in therapy, particularly for the treatment and prophylaxis of CNS disorders such as anxiety and epilepsy.

PROCESS FOR PREPARING PYRIDINE DERIVATIVES

PREPARATION OF 2-AND 4-ALKOXYCARBONYL THIOLAN-3-ONES

PURPOSE: To prepare with high yield and high purity the titled compd. being useful as an intermediate for medicines and sweetenings by a method wherein Deakman cyclization of 3-alkoxycarbonylmethylthiopropionate is performed by using a lithium alkoxide. CONSTITUTION: Cyclization of a compd. of formula I (wherein COOR is an ester functional group) is performed in the presence of a lithium alkoxide and furthermore, if necessary, a lithium salt or salts obtd. are acidified to obtain a compd. of formula II or formula III or a mixture thereof. E.g., when the reaction is performed at 50°C or lower and for a short time, the compd. of formula III is obtd. and when the reaction is performed under a condition of at least 50°C and/or at least for 3 hr, the compd. of formula II is obtd. For obtaining either the compd. of formula II or the compd. of formula III alone or the mixture thereof like these, The reaction is performed by selecting appropriately the reaction time and temp. Lithium alkoxide is ...

Azetidinecarboxamide derivatives for treating CNS disorders

A compound of formula (1), wherein: R1 is aryl; R2 is H, alkyl or aryl; and R3 is hydrogen or alkyl; pharmaceutically acceptable addition compounds thereof; and the use of the compounds in therapy, particularly for the treatment and prophylaxis of CNS disorders such as anxiety and epilepsy.

NEW PROCEDURES AND INTERMEDIARIES FOR THE PREPARATION OF PIPERAZINE DERIVATIVES.

COMPUESTOS QUE TIENEN LA FORMULA R 5 O-A-NR 4 -R SUP,2} (V), DONDE R{SUP,2} ES UN GRUPO HETEROARILICO ENLAZADO AL RESIDUO DE LA MOLECULA MEDIANTE UN ATOMO DE CARBONO ADYACENTE A UN ATOMO DE NITROGENO Y R{SUP,4} Y R{SUP,5} SON ATOMOS DE HIDROGENO O JUNTOS REPRESENTAN -SO- O -SO{SUB,2}- Y A ES ALQUILENO C{SUB,2}C{SUB,4} OPCIONALMENTE SUSTITUIDO POR UNO O MAS GRUPOS DE ALQUILO BAJO SON NUEVOS INTERMEDIARIOS EN LA PREPARACION DE DERIVADOS DE PIPERAZINA FARMACEUTICAMENTE UTIL COMO COMPUESTOS FINALES. LOS COMPUESTOS QUE TIENEN LA FORMULA GENERAL (V) DONDE R{SUP,4} Y R{SUP,5} SON HIDROGENO PUEDEN SER PREPARADOS MEDIANTE UNA REDISPOSICION DE UN COMPUESTO QUE TIENE LA FORMULA R{SUP,2}-O-ANH{SUB,2} (VI). COMPOUNDS THAT HAVE FORMULA R 5 OA-NR 4 -R SUP, 2} (V), WHERE R {SUP, 2} IS A HETEROARILICO GROUP LINKED TO THE MOLECULA WASTE THROUGH A CARBON ATOM ADJUSTMENT TO A NITROGEN YR ATOM {SUP, 4} YR {SUP, 5} ARE HYDROGEN ATOMS OR TOGETHER REPRESENT -SO- OR -SO {SUB, 2} - IT'S ALREADY RENTED C {SUB, 2} C {SUB, 4} OPTIONALLY REPLACED BY ONE OR MORE LOW RENT GROUPS ARE NEW INTERMEDIARIES IN THE PREPARATION OF PHARMACEUTICALLY USEFUL PIPERAZINE DERIVATIVES AS FINAL COMPOUNDS. THE COMPOUNDS THAT HAVE THE GENERAL FORMULA (V) WHERE R {SUP, 4} YR {SUP, 5} ARE HYDROGEN CAN BE PREPARED BY A REDISPOSITION OF A COMPOUND THAT HAS THE FORM R {SUP, 2} -O-ANH {SUB , 2} (VI).

Process for the preparation of alpha-aryl-gamma-butyrolactones

A process for preparing a lactone of general formula (I), where R is an optionally substituted phenyl group or an optionally substituted mono- or bicyclic heteroaryl radical which process comprises reacting an anion of a malonate of formula (II) with an ethylene compound of formula (III) Y-CH2-CH2OZ, to give a compound of formula (IV) and hydrolysing the compound of formula (IV) to give a lactone of formula (I). The lactones are of use as intermediates for preparing 5-HT1A binding agents.

Azetidinecarboxamide derivatives for treating cns disorders

A compound of formula (1), wherein: R1 is aryl; R2 is H, alkyl or aryl; and R3 is hydrogen or alkyl; pharmaceutically acceptable addition compounds thereof; and the use of the compounds in therapy, particularly for the treatment and prophylaxis of CNS disorders such as anxiety and epilepsy.

Azetidinecarboxamide derivatives for treating cns disorders

A compound of formula (1), wherein: R1 is aryl; R2 is H, alkyl or aryl; and R3 is hydrogen or alkyl; pharmaceutically acceptable addition compounds thereof; and the use of the compounds in therapy, particularly for the treatment and prophylaxis of CNS disorders such as anxiety and epilepsy.

Patent GR77800B

Processes and intermediates for the preparation of piperazine derivatives

Compounds having the formula R.sup.5 O--A--NR.sup.4 --R.sup.2 (V) where R 2 is a heteroaryl group linked to the remainder of the molecule via a carbon atom adjacent a nitrogen atom and R 4 and R 5 are both hydrogen atoms or together represent --SO-- or --SO 2 -- and A is C 2 -C 4 alkylene optionally substituted by one or more lower alkyl groups are novel intermediates in the preparation of pharmaceutically useful piperazine derivatives as end compounds. The compounds having formula V where R 4 and R 5 are hydrogen may be prepared by a rearrangement of a compound having the formula (VI). R.sup.2 O--A--NH.sub.2 (VI)

PROCEDURE FOR THE PREPARATION OF ALFA-ARIL-GAMMA-BUTIROLACTONAS.

UN PROCESO PARA LA PREPARACION DE UNA LACTONA DE FORMULA GENERAL (I), DONDE R ES UN GRUPO FENILO OPCIONALMENTE SUSTITUIDO O UN RADICAL HETEROARILO MONO- O BICICLICO OPCIONALMENTE SUSTITUIDO CUYO PROCESO COMPRENDE LA REACCION DE UN ANION DE UN MALONATO DE FORMULA (II) CON UN COMPUESTO DE ETILENO DE FORMULA (III) Y-CH2-CH2OZ, PARA PROPORCIONAR UN COMPUESTO DE FORMULA (IV) Y LA HIDROLIZACION DEL COMPUESTO DE FORMULA (IV) PARA PROPORCIONAR UNA LACTONA DE FORMULA (I). LAS LACTONAS SON DE USO COMO COMPUESTOS PARA LA PREPARACION DE AGLUTINANTES 5-HT1A. A PROCESS FOR THE PREPARATION OF A LACTONE OF GENERAL FORMULA (I), WHERE R IS AN OPTIONALLY SUBSTITUTED PHENYLIC GROUP OR AN OPTIONALLY SUBSTITUTED MONO- OR BICYCLE RADICAL WHOSE PROCESS INCLUDES THE REACTION OF AN ANION OF A MALONATE OF FORMULA AN ETHYLENE COMPOUND OF FORMULA (III) AND-CH2-CH2OZ, TO PROVIDE A COMPOUND OF FORMULA (IV) AND THE HYDROLYZATION OF THE FORMULA COMPOUND (IV) TO PROVIDE A FORMULA LACTONE (I). LACTONES ARE FOR USE AS COMPOUNDS FOR THE PREPARATION OF BINDERS 5-HT1A.

DERIVATIVES OF AZETIDINOCARBOXAMIDE FOR THE TREATMENT OF DISORDERS OF THE CENTRAL NERVOUS SYSTEM.

Un compuesto de fórmula (1) en la que R1 es arilo sustituido con grupos sustituyentes seleccionados entre halo y haloalquilo; y R2 es hidrógeno o alquilo. A compound of formula (1) in which R 1 is aryl substituted with substituent groups selected from halo and haloalkyl; and R2 is hydrogen or alkyl.

AZETIDINOCARBOXAMIDE DERIVATIVES FOR THE TREATMENT OF CNS DISTURBACTIONS

Azetidinecarboxamide derivatives for treating cns disorders

A compound of formula (1) wherein R<1 >is aryl; and R<2 >is hydrogen or alkyl; pharmaceutically acceptable addition compounds thereof; and their use in therapy, particularly for the treatment and prophylaxis of CNS disorders such as anxiety and epilepsy.

Azetidinecarboxamide derivatives for treating cns disorders

A compound of formula (1), wherein: R1 is aryl; R2 is H, alkyl or aryl; and R3 is hydrogen or alkyl; pharmaceutically acceptable addition compounds thereof; and the use of the compounds in therapy, particularly for the treatment and prophylaxis of CNS disorders such as anxiety and epilepsy.

Novel processes and intermediates for the preparation of piperazine derivatives

Verfahren und zwischenprodukte zur herstellung von piperazinderivaten

Azetidincarboxamidderivate zur behandlung von zns-erkrankungen

Verfahren zur herstellung von pyridinderivaten.

Meta-hydroxyphenyl-substituierte verbindungen.

Preparation of cyclohexanol derivatives and novel thioamide intermediates

Preparation of cyclohexanol derivatives and novel thioamide intermediates

Azetidincarboxamidderivate zur behandlung von zns-erkrankungen

Azetidinecarboxamide derivatives for treating cns disorders

A compound of formula (1) wherein R<1 >is aryl; and R<2 >is hydrogen or alkyl; pharmaceutically acceptable addition compounds thereof; and their use in therapy, particularly for the treatment and prophylaxis of CNS disorders such as anxiety and epilepsy.

Procedimiento para la preparacion de derivados de hezahidroacepina,piperidina o pirrolidina