CH301585A - Process for the preparation of a new thioketopiperidine. - Google Patents

Process for the preparation of a new thioketopiperidine.

Info

Publication number
CH301585A
CH301585A CH301585DA CH301585A CH 301585 A CH301585 A CH 301585A CH 301585D A CH301585D A CH 301585DA CH 301585 A CH301585 A CH 301585A
Authority
CH
Switzerland
Prior art keywords
thioketopiperidine
ethyl
new
phenyl
preparation
Prior art date
Application number
Other languages
German (de)
Inventor
Aktiengesellschaft Ciba
Original Assignee
Ciba Geigy
Priority date (The priority date is an assumption and is not a legal conclusion. Google has not performed a legal analysis and makes no representation as to the accuracy of the date listed.)
Filing date
Publication date
Application filed by Ciba Geigy filed Critical Ciba Geigy
Publication of CH301585A publication Critical patent/CH301585A/en

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Description

  

  verfahren zur Herstellung eines neuen     Thioketopiperidins.            (Tegenstand    des vorliegenden Patentes ist  ein Verfahren zur Herstellung eines     Thioketo-          piperidins,    welches dadurch gekennzeichnet  ist, dass man     3-Phenyl-3-ät.hyl-2,6-dioxo-          piperidin    mit einem Sauerstoff durch Schwe  fel ersetzenden     l-Iittel    behandelt.  



  Das so erhaltene     3-Pheny        1-3-äthyl-2-oxo-6-          tliioketopiperidin    der Formel  
EMI0001.0011     
    vom F. = 73 bis 75  ist neu. Es besitzt     anti-          eonvulsive    Wirksamkeit und soll als Heilmittel       Verwendung    finden.  



  Als Sauerstoff durch Schwefel ersetzendes  Mittel verwendet man zweckmässig     Phosphor-          pentasulfid,    vorzugsweise in Gegenwart eines  Verdünnungsmittels, wie     Pyridin.     



       Beispiel:     20     (Tewiehtsteile        3-Plienyl-3-ät.hyl-2,6-dioxo-          l)iperidinwerden        init120        Voluniteilenabsolutem          Pyridin    und 20     (lewichtsteilen    fein pulverisier  tem     Pliospliorpentasulfid    unter gutem Rühren  während 2 Stunden am     Rückfluss    gekocht und  hierauf das heisse Reaktionsgemisch in 1000       Volumteile    heissen Wassers eingetragen.

   Nach  dem Abkühlen wird das Ganze mit Essigester       eisschöpfend    extrahiert, der     Essigesterauszug     mit verdünnter     Sodalösung,    verdünnter Salz-         säure    und schliesslich mit Wasser gewaschen,  über     Calciumchlorid    getrocknet und das Lö  sungsmittel abgedampft. Der Rückstand, be  stehend aus     3-Phenyl-3-äthyl-2-oxo-6-thioketo-          piperidin    der Formel  
EMI0001.0036     
    wird im Hochvakuum     destilliert    und geht über  bei 159 bis 162  (0,12 mm).

   Beim Stehen kri  stallisiert diese Verbindung und zeigt, umkri  stallisiert aus Essigester unter Zusatz von       Ligroin,    einen F. von 73 bis 75 .



  process for the production of a new thioketopiperidine. (The subject matter of the present patent is a process for the production of a thioketopiperidine, which is characterized in that 3-phenyl-3-ethyl-2,6-dioxopiperidine is treated with a sulfur-replacing agent .



  The 3-Pheny 1-3-ethyl-2-oxo-6-tliioketopiperidin of the formula obtained in this way
EMI0001.0011
    vom F. = 73 to 75 is new. It has anti-eonvulsive effectiveness and is said to be used as a remedy.



  The sulfur-replacing agent used is advantageously phosphorus pentasulfide, preferably in the presence of a diluent such as pyridine.



       Example: 20 parts by weight of 3-plienyl-3-ethyl-2,6-dioxol) iperidine are refluxed with 120 parts by volume of absolute pyridine and 20 parts by weight of finely pulverized pliosplior pentasulfide with thorough stirring for 2 hours and then the hot reaction mixture in 1000 parts by volume of hot water entered.

   After cooling, the whole thing is extracted with ice-scooping ethyl acetate, the ethyl acetate extract is washed with dilute soda solution, dilute hydrochloric acid and finally with water, dried over calcium chloride and the solvent is evaporated off. The residue, consisting of 3-phenyl-3-ethyl-2-oxo-6-thioketopiperidine of the formula
EMI0001.0036
    is distilled in a high vacuum and goes over at 159 to 162 (0.12 mm).

   This compound crystallizes on standing and shows, umkri crystallized from ethyl acetate with the addition of ligroin, a F. of 73 to 75.

 

Claims (1)

PATENTANSPRUCH: Verfahren zur Herstellung eines neuen Thioketopiperidins, dadurch gekennzeichnet, da.ss man 3-Phenyl-3-äthyl-2,6-dioxo-piperidin mit einem Sauerstoff durch Schwefel ersetzen den Mittel behandelt. Das so erhaltene 3-Phenyl-3-äthyl-2-oxo-6- thioketopiperidin der Formel EMI0001.0044 vom F. = 73 bis 75 besitzt anticonvulsive Wirksamkeit und soll als Heilmittel Verwen dung finden. UNTERANSPRÜCHE: 1. PATENT CLAIM: Process for the production of a new thioketopiperidine, characterized in that 3-phenyl-3-ethyl-2,6-dioxo-piperidine is treated with an oxygen by sulfur substituting the agent. The 3-phenyl-3-ethyl-2-oxo-6-thioketopiperidine of the formula obtained in this way EMI0001.0044 vom F. = 73 to 75 has anticonvulsant effectiveness and is said to be used as a remedy. SUBCLAIMS: 1. Verfahren nach Patentanspruch, da durch gekennzeichnet, dass man als Sauer- Stoff durch Schwefel ersetzendes Mittel Phos- phorpentasulfid verwendet. 2. Verfahren nach Patentanspruch und Unteranspruch 1, dadurch gekennzeichnet, dass man das 3-Phenyl-3-äthyl-2,6-dioxo-piperidin in Gegenwart eines Verdünnungsmittels mit dem Phosphorpentasulfid behandelt. Process according to patent claim, characterized in that phosphorus pentasulphide is used as the oxygen substance which replaces sulfur. 2. The method according to claim and dependent claim 1, characterized in that treating the 3-phenyl-3-ethyl-2,6-dioxo-piperidine in the presence of a diluent with the phosphorus pentasulfide.
CH301585D 1952-04-03 1951-04-28 Process for the preparation of a new thioketopiperidine. CH301585A (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CH301585T 1952-04-03

Publications (1)

Publication Number Publication Date
CH301585A true CH301585A (en) 1954-09-15

Family

ID=4491095

Family Applications (1)

Application Number Title Priority Date Filing Date
CH301585D CH301585A (en) 1952-04-03 1951-04-28 Process for the preparation of a new thioketopiperidine.

Country Status (1)

Country Link
CH (1) CH301585A (en)

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