CH242520A - Process for the preparation of an acylated sulfonamide. - Google Patents

Process for the preparation of an acylated sulfonamide.

Info

Publication number
CH242520A
CH242520A CH242520DA CH242520A CH 242520 A CH242520 A CH 242520A CH 242520D A CH242520D A CH 242520DA CH 242520 A CH242520 A CH 242520A
Authority
CH
Switzerland
Prior art keywords
amino
dimethyl
sulfonamide
benzene
preparation
Prior art date
Application number
Other languages
German (de)
Inventor
Ag J R Geigy
Original Assignee
Ag J R 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 Ag J R Geigy filed Critical Ag J R Geigy
Publication of CH242520A publication Critical patent/CH242520A/en

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Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07CACYCLIC OR CARBOCYCLIC COMPOUNDS
    • C07C311/00Amides of sulfonic acids, i.e. compounds having singly-bound oxygen atoms of sulfo groups replaced by nitrogen atoms, not being part of nitro or nitroso groups
    • C07C311/15Sulfonamides having sulfur atoms of sulfonamide groups bound to carbon atoms of six-membered aromatic rings

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)

Description

  

  Verfahren zur Herstellung eines     acylierten    Sulfonamides.    Gegenstand vorliegenden Patentes ist ein  Verfahren zur Herstellung eines     acylierten     Sulfonamides. Das Verfahren ist dadurch       gekennzeichnet,    dass man ein substituiertes       4-Amino-benzolsulfonamid        der    Formel  
EMI0001.0006     
    in der R einen durch     hydrolysierende        Mittel          abspaltbaren    Rest bedeutet, durch     Verseifung     in     4-Amino-benzol-N,-(.a,ss-dimethyl-cro-          tonoyl)=sulfonamid    überführt.  



  Die neue     Verbindung    bildet farblose Kri  stalle vom     Schmelzpunkt    160-162 . Sie soll  als     Arzneimittel        Verwendung        finden.     



  <I>Beispiel 1:</I>  10 Teile     N-(4-Amino-benzolsulfonyl)-a,ss-          dimethyl    -     crotonsäureamidin    vom Schmelz  punkt 168-169  und der Formel  
EMI0001.0021     
    werden mit 200 Teilen 3,5 %     iger    Salzsäure  20 Stunden auf 90-100  erhitzt. Nach dem  Erkalten wird     sodaalkalisch    gestellt, filtriert       und        mit    Essigsäure angesäuert. Man erhält  das     4-Amino-benzol-N,-(a,ss-dimethyl-cro-          tonoyl)-sulfonamid.    Aus Alkohol umkristal  lisiert bildet es farblose Kristalle vom  Schmelzpunkt 160-162 .

      <I>Beispiel 2:</I>  10 Teile     N-(4-Amino-benzolsulfonyl)-a,ss-          dimethyl    -     crotonsäure    -     iminoäthyläther    vom       Schmelzpunkt    150-151  und der Formel  
EMI0001.0033     
      werden mit 200 Teilen 3,5     joiger    Salzsäure  4     Stunden    auf 90-100  erhitzt. Nach dem       Erkalten    wird     sodaalkalisch    gestellt,     filtriert     und mit     Essigsäure    angesäuert.

   Man erhält  das     4-Amino-benzol-N,.-(a,ss-dimethyl-cro-          tonoyl)-sulfonamid.    Aus Alkohol umkristal  lisiert     bildet    es farblose Kristalle vom       Schmelzpunkt    160-162 .



  Process for the preparation of an acylated sulfonamide. The present patent relates to a process for the preparation of an acylated sulfonamide. The process is characterized in that a substituted 4-amino-benzenesulfonamide of the formula
EMI0001.0006
    in which R denotes a radical that can be split off by hydrolyzing agents, converted by saponification into 4-amino-benzene-N, - (. a, ss-dimethyl-cotonoyl) = sulfonamide.



  The new compound forms colorless crystals with a melting point of 160-162. It should be used as a medicine.



  <I> Example 1: </I> 10 parts of N- (4-amino-benzenesulfonyl) -a, ss- dimethyl-crotonic acid amidine with a melting point of 168-169 and the formula
EMI0001.0021
    are heated to 90-100 for 20 hours with 200 parts of 3.5% hydrochloric acid. After cooling, it is made alkaline with soda, filtered and acidified with acetic acid. The 4-amino-benzene-N, - (α, ß-dimethyl-cotonoyl) -sulfonamide is obtained. Recrystallized from alcohol, it forms colorless crystals with a melting point of 160-162.

      <I> Example 2: </I> 10 parts of N- (4-amino-benzenesulfonyl) -a, ss- dimethyl-crotonic acid-iminoethyl ether with a melting point of 150-151 and the formula
EMI0001.0033
      are heated to 90-100 for 4 hours with 200 parts of 3.5 hydrochloric acid. After cooling, it is made alkaline with soda, filtered and acidified with acetic acid.

   The 4-amino-benzene-N, .- (a, ss-dimethyl-cotonoyl) -sulfonamide is obtained. Recrystallized from alcohol, it forms colorless crystals with a melting point of 160-162.

 

Claims (1)

PATENTANSPRUCH: Verfahren zur Herstellung eines acylier- ten Sulfonamides, dadurch gekennzeichnet, dass man ein substituiertes 4-Amino-benzol- sulfonamid der Formel EMI0002.0018 in der R einen durch hydrolysierende:llIittel abspaltbaren Rest bedeutet, durch Verseifung in 4-Amino-benzol-Nl-,(a,ss-dimethyl-cro- tonoyl)-sulfonamid überführt. PATENT CLAIM: Process for the preparation of an acylated sulfonamide, characterized in that a substituted 4-amino-benzenesulfonamide of the formula EMI0002.0018 in which R denotes a radical which can be split off by hydrolyzing agents, converted by saponification into 4-amino-benzene-Nl -, (α, ß-dimethyl-cotonoyl) -sulfonamide. Die neue Verbindung bildet farblose Kri- stalle vom Schmelzpunkt 160-162 . Sie E21- als Arzneimittel Verwendung finden. <B>UNTERANSPRÜCHE:</B> 1. The new compound forms colorless crystals with a melting point of 160-162. You can use E21 as a medicinal product. <B> SUBClaims: </B> 1. Verfahren nach Patentanspruch, da durch gekennzeichnet, dass man N-(4-Amino- benzolsulfonyl) <I>-</I> a,ss <I>-</I> dimethyl - crotonsäure- amidiu durch hydrolytische Spa-ltung in 4-Amino - benzol-Nl-(a, ss-dimethyl-crotssnoyl)- sulfonamid überführt. 2. Process according to claim, characterized in that N- (4-aminobenzenesulfonyl) <I> - </I> a, ss <I> - </I> dimethyl - crotonic acid amide by hydrolytic cleavage in 4 - Amino - benzene-Nl- (a, ss-dimethyl-crotssnoyl) - sulfonamide transferred. 2. Verfahren nach Patentanspruch, - da durch gekennzeichnet, dass man N=(4-Amino- benzolsulfonyl) <I>-</I> ass<I>-</I> dimethyl - crotonsäure- iminoäthyläther durch hydrolytische Spal tung in 4-Amino-benzol-Nl-(a,ss-dimpthyl- crotonoyl)-sulfonamid überführt. Process according to patent claim, characterized in that N = (4-aminobenzenesulfonyl) <I> - </I> ass <I> - </I> dimethyl - crotonic acid iminoethyl ether by hydrolytic cleavage into 4-amino -benzene-Nl- (a, ss-dimpthyl-crotonoyl) -sulfonamid transferred.
CH242520D 1943-05-21 1943-05-21 Process for the preparation of an acylated sulfonamide. CH242520A (en)

Applications Claiming Priority (2)

Application Number Priority Date Filing Date Title
CH242520T 1943-05-21
CH239850T 1944-03-16

Publications (1)

Publication Number Publication Date
CH242520A true CH242520A (en) 1946-05-15

Family

ID=25728449

Family Applications (1)

Application Number Title Priority Date Filing Date
CH242520D CH242520A (en) 1943-05-21 1943-05-21 Process for the preparation of an acylated sulfonamide.

Country Status (1)

Country Link
CH (1) CH242520A (en)

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