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MC897A1 - Process for the preparation of N-Ú (ethyl-1-pyrrolidinyl-2) methyl¾ methoxy-2-sulfamoyl-5-benzamide - Google Patents

Process for the preparation of N-Ú (ethyl-1-pyrrolidinyl-2) methyl¾ methoxy-2-sulfamoyl-5-benzamide

Info

Publication number
MC897A1
MC897A1 MC956A MC956A MC897A1 MC 897 A1 MC897 A1 MC 897A1 MC 956 A MC956 A MC 956A MC 956 A MC956 A MC 956A MC 897 A1 MC897 A1 MC 897A1
Authority
MC
Monaco
Prior art keywords
methoxy
ethyl
sulfamoyl
pyrrolidinyl
benzamide
Prior art date
Application number
MC956A
Other languages
French (fr)
Inventor
F Kuenzy
Original Assignee
Fratmann Sa
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 Fratmann Sa filed Critical Fratmann Sa
Publication of MC897A1 publication Critical patent/MC897A1/en

Links

Classifications

    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07FACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAINING ELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN, SULFUR, SELENIUM OR TELLURIUM
    • C07F9/00Compounds containing elements of Groups 5 or 15 of the Periodic Table
    • C07F9/02Phosphorus compounds
    • C07F9/547Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom
    • C07F9/553Heterocyclic compounds, e.g. containing phosphorus as a ring hetero atom having one nitrogen atom as the only ring hetero atom
    • C07F9/572Five-membered rings
    • CCHEMISTRY; METALLURGY
    • C07ORGANIC CHEMISTRY
    • C07DHETEROCYCLIC COMPOUNDS
    • C07D207/00Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom
    • C07D207/02Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom
    • C07D207/04Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members
    • C07D207/08Heterocyclic compounds containing five-membered rings not condensed with other rings, with one nitrogen atom as the only ring hetero atom with only hydrogen or carbon atoms directly attached to the ring nitrogen atom having no double bonds between ring members or between ring members and non-ring members with hydrocarbon radicals, substituted by hetero atoms, attached to ring carbon atoms
    • C07D207/09Radicals substituted by nitrogen atoms, not forming part of a nitro radical

Landscapes

  • Chemical & Material Sciences (AREA)
  • Organic Chemistry (AREA)
  • Health & Medical Sciences (AREA)
  • Life Sciences & Earth Sciences (AREA)
  • Biochemistry (AREA)
  • General Health & Medical Sciences (AREA)
  • Molecular Biology (AREA)
  • Low-Molecular Organic Synthesis Reactions Using Catalysts (AREA)
  • Pharmaceuticals Containing Other Organic And Inorganic Compounds (AREA)
  • Pyrrole Compounds (AREA)

Description

BREVET D'INVENTION PATENT FOR INVENTION

.Procède de préparation du N- jjéthyl-l-pyrrolidinyl-2)- méthylj -méthoxy- 2-sulfamoyl-5-benzamide Process for preparing N-ethyl-1-pyrrolidinyl-2-methyl-2-methoxy-sulfamoyl-5-benzamide

FRATMANN S.A. FRATMANN S.A.

La présente invention concerne un procédé de préparation du N-£ (éthyl-l-pyrrolidinyl- 2) -méthyl J -méthoxy-2-sulfamoyl-5-benzamide à partir d'acide méthoxy-2-sulfamoyl-5-benzoi"que et d'éthyl-1-aminométhyl-2-pyrrolidinë permettant d'obtenir un très bon rendement. The present invention relates to a process for preparing N-Σ (ethyl-1-pyrrolidinyl-2)-methyl α-methoxy-2-sulfamoyl-5-benzamide from methoxy-2-sulfamoyl-5-benzoic acid and ethyl-1-aminomethyl-2-pyrrolidin, allowing for a very good yield.

Le procédé selon l'invention est caractérisé essentiellement en ce que l'on fait réagir l'acide méthoxy-2-sulfamoyl-5-benzoi'que et l'éthyl-1-aminométhyl-2-pyrrolidine en présence de trichlorure de phosphore. The process according to the invention is characterized essentially in that methoxy-2-sulfamoyl-5-benzoic acid and ethyl-1-aminomethyl-2-pyrrolidine are reacted in the presence of phosphorus trichloride.

Comme milieu de réaction on utilise de préférence la pyridine. Pyridine is preferably used as the reaction medium.

La réaction-se produit selon le schéma suivant ch2nh2 The reaction occurs according to the following scheme: ch2nh2

C2 H5 C2 H5

+ pcl r + pcl r

ch N = p ch N = p

_ NH-CH _ NH-CH

C H 2 5 CH25

2 —N^^ 2 —N^^

I I

C2H5 C2H5

+ +

CH30' CH30'

S02NH2 SO2NH2

COOH COOH

CH3O CH3O

S°2NH2 S°2NH2

CONH- CH F CONH- CH F

L I L I

C2H5 C2H5

3. 3.

L'exemple suivant est donné pour illustrer l'invention : The following example is given to illustrate the invention:

Dans un ballon d'un litre muni d'un agitateur, d'un réfrigérant ascendant, d'un thermomètre et d'une ampoule à brome, on introduit 27g (0,11 mpl) d'éthyl-l-aminométhyl-2-pyrrolidine et 560 ml de pyridine. 5 On agite la solution obtenue et verse goutte à goutte 5, 6 g de trichlo- In a one-liter flask equipped with a stirrer, a rising condenser, a thermometer, and a bromine funnel, 27 g (0.11 µL) of ethyl-1-aminomethyl-2-pyrrolidine and 560 mL of pyridine are introduced. The resulting solution is stirred, and 5.6 g of trichloro-

rure de phosphore (0, 04 mol) dissout dans 64 ml de pyridine tout en maintenant la température vers 20°C. Phosphorus ride (0.04 mol) dissolved in 64 ml of pyridine while maintaining the temperature around 20°C.

On laisse agiter l/2 heure à 20°C et on ajoute 14, 8 g (0, 064 mol) d'acide méthoxy-2-sulfamoyl-5-benzoi'que. On chauffe le mélange à reflux durant 4 l/2 heures et laisse reposer une nuit. La pyridine est ensuite chassée sous vide et le résidu est extrait par 200 ml d'acide chiorhydrique à 10 %. On obtient un précipité qui est chauffé vers 70-80°C et qui se dissout. Cette solution est traitée par 15 ml d'ammoniaque concentré. Le précipité formé est filtré, lavé à l'eau et séché à l'étuve à 50°C. The mixture is stirred for 30 minutes at 20°C, and 14.8 g (0.064 mol) of 2-methoxy-5-sulfamoylbenzoic acid is added. The mixture is heated under reflux for 4.5 hours and left to stand overnight. The pyridine is then removed under vacuum, and the residue is extracted with 200 mL of 10% hydrochloric acid. A precipitate is obtained, which is heated to approximately 70-80°C and dissolves. This solution is treated with 15 mL of concentrated ammonia. The resulting precipitate is filtered, washed with water, and dried in an oven at 50°C.

On obtient 16, 2 g (rendement de 74, 3 %) de N- £ (éthyl-l-pyrrolidinyl-2)- méthyl J -méthoxy~2-sulfamoyl~5-benzamide avec un point de fusion de 178° C. We obtain 16.2 g (yield of 74.3%) of N-Σ(ethyl-l-pyrrolidinyl-2)-methyl J-methoxy~2-sulfamoyl~5-benzamide with a melting point of 178° C.

Le N- j~(éthyl-l-pyrrolidinyl-2)- méthyl J -méthoxy-2-sulfamoyl-5-» 20 • ' benzamide constitue un produit intermédiaire, permettant la fabrication de principes actifs utilisables, notamment dans l'industrie phar-i ■ N-(ethyl-1-pyrrolidinyl-2)-methyl-2-methoxy-5-sulfamoyl benzamide constitutes an intermediate product, enabling the manufacture of usable active ingredients, particularly in the pharmaceutical industry.

maceutique et particulièrement en gastro-entérologie et en neurologie. / macumatics, particularly in gastroenterology and neurology.

10 10

15 15

Claims (1)

'H' \*-r'H' \*-r ■JN' *-■JN' *- ''If ^''If ^ fT/ï-.fT/ï-. . t-ty". "■ V. t-ty". "■ V <*: :K<*: :K '"«i|s^ÉiiÉiip3;sr 's asfSiS||alB#S«\:;s *'"«i|s^ÉiiÉiip3;sr 's asfSiS||alB#S«\:;s * u'i"' /*■»,"Su'i"' /*■","S resume 'summary ' (.(. L'invention a pour objet :The purpose of the invention is: Un procédé de préparation du N- £ (éthyl-l-pyrrolidinyl~ 2)-méthyl J -méthoxy-2-sulfamoyl-5-benzamide caractérisé par les points sui-vants considérés isolément ou en combinaison :A process for preparing N-Σ(ethyl-1-pyrrolidinyl~2)-methyl-2-methoxy-5-sulfamoylbenzamide characterized by the following points considered individually or in combination: On fait réagir l'acide méthoxy-2-sulfamoyl-5-benzoi'que et l'éthyl-l-aminbméthyl-2-pyrrolidine en présence de trichlorure de phosphore.2-Methoxy-2-sulfamoyl-5-benzoic acid and ethyl-1-aminomethyl-2-pyrrolidine are reacted in the presence of phosphorus trichloride. On utilise la pyridine comme milieu de réaction.Pyridine is used as the reaction medium. 99 =<-w(r {*_ /^<30V', r^s^.6 9^-=<-w(r {*_ /^<30V', r^s^.6 9^- Pau* ProcuratlefiPau* Procuratlefi ûû Jf vd *Jf vd * /^s^Ay t ,/^s^Ay t ,
MC956A 1971-08-20 1971-11-09 Process for the preparation of N-Ú (ethyl-1-pyrrolidinyl-2) methyl¾ methoxy-2-sulfamoyl-5-benzamide MC897A1 (en)

Applications Claiming Priority (1)

Application Number Priority Date Filing Date Title
CH1226771A CH547797A (en) 1971-08-20 1971-08-20 PROCESS FOR THE PREPARATION OF N - ((1-AETHYL-PYRROLIDINYL2) -METHYL) -2-METHOXY-5-SULFAMOYL-BENZAMIDE.

Publications (1)

Publication Number Publication Date
MC897A1 true MC897A1 (en) 1972-06-22

Family

ID=4381427

Family Applications (1)

Application Number Title Priority Date Filing Date
MC956A MC897A1 (en) 1971-08-20 1971-11-09 Process for the preparation of N-Ú (ethyl-1-pyrrolidinyl-2) methyl¾ methoxy-2-sulfamoyl-5-benzamide

Country Status (26)

Country Link
JP (1) JPS4829764A (en)
KR (1) KR780000067B1 (en)
AT (1) AT311328B (en)
BE (1) BE774104A (en)
CA (1) CA928714A (en)
CH (1) CH547797A (en)
CS (1) CS177818B2 (en)
DE (1) DE2152370A1 (en)
DK (1) DK126325B (en)
ES (1) ES396718A1 (en)
FR (1) FR2111372A5 (en)
GB (1) GB1328747A (en)
HU (1) HU166567B (en)
IE (1) IE35821B1 (en)
IL (1) IL38098A (en)
LU (1) LU64275A1 (en)
MC (1) MC897A1 (en)
NL (1) NL7114902A (en)
NO (1) NO136460C (en)
OA (1) OA03928A (en)
PL (1) PL84446B1 (en)
RO (1) RO62479A (en)
SE (1) SE376914B (en)
YU (1) YU34286B (en)
ZA (1) ZA717543B (en)
ZM (1) ZM17771A1 (en)

Families Citing this family (4)

* Cited by examiner, † Cited by third party
Publication number Priority date Publication date Assignee Title
FR2252336B1 (en) * 1973-11-27 1977-03-04 Ile De France
JPS5170235A (en) * 1974-12-16 1976-06-17 Toyo Aluminium Kk
NZ186175A (en) * 1977-01-27 1980-03-05 Shionogi & Co Meta-sulphonamidobenzamide derivatives
WO1991017144A1 (en) * 1990-05-02 1991-11-14 Yoshitomi Pharmaceutical Industries, Ltd. Amide compound, pharmaceutical use thereof and novel 1-substituted pyrrolidinemethyl-amines

Also Published As

Publication number Publication date
DE2152370A1 (en) 1973-02-22
NO136460B (en) 1977-05-31
PL84446B1 (en) 1976-04-30
HU166567B (en) 1975-04-28
ES396718A1 (en) 1974-05-16
NL7114902A (en) 1973-02-22
CA928714A (en) 1973-06-19
IL38098A (en) 1974-12-31
SE376914B (en) 1975-06-16
IE35821L (en) 1973-02-20
AU3572171A (en) 1973-05-24
LU64275A1 (en) 1972-06-02
FR2111372A5 (en) 1972-06-02
CH547797A (en) 1974-04-11
NO136460C (en) 1977-09-07
RO62479A (en) 1978-02-15
CS177818B2 (en) 1977-08-31
DK126325B (en) 1973-07-02
GB1328747A (en) 1973-08-30
YU282171A (en) 1978-10-31
KR780000067B1 (en) 1978-03-30
BE774104A (en) 1972-04-18
JPS4829764A (en) 1973-04-19
YU34286B (en) 1979-04-30
ZM17771A1 (en) 1972-08-21
OA03928A (en) 1975-08-14
IE35821B1 (en) 1976-05-26
AT311328B (en) 1973-11-12
ZA717543B (en) 1972-08-30
IL38098A0 (en) 1972-01-27

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