MX3141E - PROCEDURE TO PREPARE BENCIL AMINAS - Google Patents

PROCEDURE TO PREPARE BENCIL AMINAS

Info

Publication number
MX3141E
MX3141E MX360873U MX360873U MX3141E MX 3141 E MX3141 E MX 3141E MX 360873 U MX360873 U MX 360873U MX 360873 U MX360873 U MX 360873U MX 3141 E MX3141 E MX 3141E
Authority
MX
Mexico
Prior art keywords
carbon atoms
radical
group
signifies
hydrogen atom
Prior art date
Application number
MX360873U
Other languages
Spanish (es)
Inventor
Klaus Renhold Noll
Johannes Keck
Sigfrid Puschmann
Gerd Kruger
Original Assignee
Thomae Gmbh Dr K
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
Priority claimed from DE2316325A external-priority patent/DE2316325A1/en
Priority claimed from DE19732320967 external-priority patent/DE2320967C3/en
Priority claimed from DE2346743A external-priority patent/DE2346743C3/en
Application filed by Thomae Gmbh Dr K filed Critical Thomae Gmbh Dr K
Publication of MX3141E publication Critical patent/MX3141E/en

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  • Organic Low-Molecular-Weight Compounds And Preparation Thereof (AREA)
  • Acyclic And Carbocyclic Compounds In Medicinal Compositions (AREA)
  • Pyrrole Compounds (AREA)
  • Heterocyclic Carbon Compounds Containing A Hetero Ring Having Nitrogen And Oxygen As The Only Ring Hetero Atoms (AREA)

Abstract

La presente invención se refiere a un procedimiento para la preparación de bencilaminas de la fórmula general I, (VER FIGURA), en la que Ha1 significa un átomo de cloro o de bromo, R1 significa un átomo de hidrógeno, cloro o bromo, R2 significa el radical morfolinocarbonilmetilo, un radical alcohilo ramificado con 3 a 5 átomos de carbono eventualmente sustituído con 1 a 3 grupos hidroxilo, o un grupo de la fórmula (VER FIGURA), en donde R3 significa un átomo de hidrógeno, un grupo hidroxi o un grupo alcohilo con 1 a 4 átomos de carbono, n significa los números 0, 1 ó 2 y los dos radicales A y B significan átomos de hidrógeno o conjuntamente el grupo (VER FIGURA), en donde R5 represente un átomo de hidrógeno o un radical alcohilo inferior con 1 o 2 átomos de carbono y m significa los números 1 ó 2, R4 significa un radical alcohilo de cadena recta o ramificada con 1 a 4 átomos de carbono, un radical alquenilo con 2 a 4 átomos de carbono, un radical cicloalcohilo con 3 ó 4 átomos de carbono o también un átomo de hidrógeno, caso que R3 no represente ningún átomo de hidrógeno o R2 represente un radical alcohilo ramificado con 3 a 5 átomos de carbono eventualmente sustituído con 1 a 3 grupos hidroxilo; y 1 significa los números 1 ó 2, así como de sus sales por adición de ácido fisiológicamente compatibles con ácidos orgánicos o inorgánicos, caracterizado porque de un compuesto de fórmula general II (VER FIGURA), en la que R1 , R2, Ha1 y 1 son como se a definido inicialmente,X representa un radical protector para un grupo amino, por ejemplo un grupo acilo o posee los significados inicialmente citados para R4, e Y representa un radical protector y un grupo hidroxilo por ejemplo un grupo acilo, alquilo arilo o en el caso en que X representa un grupo protector par un grupo amino, representa un átomo de hidrógeno, se separa uno o dos radicales y protectores en un disolvente por medio de hidrólisis a temperaturas de entre 0°C y la temperatura de ebullición del disolvente utilizado, por ejemplo a temperaturas de entre 0 y 100°C y un compuesto de la fórmula general I, obtenido de acuerdo con el procedimiento es trasnformado en caso deseado a continuación de sus sales fisiológicamente compatibles con ácidos orgánicos o inorgánicos.The present invention relates to a process for the preparation of benzylamines of the general formula I, (SEE FIGURE), in which Ha1 signifies a chlorine or bromine atom, R1 signifies a hydrogen, chlorine or bromine atom, R2 signifies the morpholinocarbonylmethyl radical, a branched alcohol radical with 3 to 5 carbon atoms, optionally substituted with 1 to 3 hydroxyl groups, or a group of the formula (SEE FIGURE), where R3 signifies a hydrogen atom, a hydroxy group or a group alcohol with 1 to 4 carbon atoms, n means the numbers 0, 1 or 2 and the two radicals A and B mean hydrogen atoms or together the group (SEE FIGURE), where R5 represents a hydrogen atom or an alcohol radical lower with 1 or 2 carbon atoms and m signifies the numbers 1 or 2, R4 signifies a straight chain or branched alcohol radical with 1 to 4 carbon atoms, an alkenyl radical with 2 to 4 carbon atoms, a cycloalcohyl radical with 3 or 4 carbon atoms not or also a hydrogen atom, in case R3 does not represent any hydrogen atom or R2 represents a branched alcohol radical with 3 to 5 carbon atoms, possibly substituted with 1 to 3 hydroxyl groups; and 1 means the numbers 1 or 2, as well as their acid addition salts physiologically compatible with organic or inorganic acids, characterized in that of a compound of general formula II (SEE FIGURE), in which R1, R2, Ha1 and 1 are as initially defined, X represents a protective radical for an amino group, for example an acyl group or has the initially mentioned meanings for R4, and Y represents a protective radical and a hydroxyl group for example an acyl, alkyl aryl or in the case where X represents a protecting group for an amino group, represents a hydrogen atom, one or two radicals and protectors are separated in a solvent by means of hydrolysis at temperatures between 0 ° C and the boiling temperature of the solvent used, for example at temperatures between 0 and 100 ° C and a compound of the general formula I, obtained according to the procedure, is transformed, if desired, after its physiologically compatible salts ible with organic or inorganic acids.

MX360873U 1973-04-02 1973-10-23 PROCEDURE TO PREPARE BENCIL AMINAS MX3141E (en)

Applications Claiming Priority (3)

Application Number Priority Date Filing Date Title
DE2316325A DE2316325A1 (en) 1972-10-23 1973-04-02 Halo-hydroxy-substd-benzylamines - as secretolytic and antitussive agents
DE19732320967 DE2320967C3 (en) 1973-04-26 New benzylamines, their physiologically acceptable salts, processes for their production and pharmaceuticals containing them
DE2346743A DE2346743C3 (en) 1972-10-23 1973-09-17 2- or 4-Hydroxy-3,5-dihalogenobenzylamines, their physiologically tolerable salts, processes for their preparation and medicaments containing them

Publications (1)

Publication Number Publication Date
MX3141E true MX3141E (en) 1980-05-06

Family

ID=27185164

Family Applications (1)

Application Number Title Priority Date Filing Date
MX360873U MX3141E (en) 1973-04-02 1973-10-23 PROCEDURE TO PREPARE BENCIL AMINAS

Country Status (5)

Country Link
AT (1) ATA88775A (en)
ES (4) ES423976A1 (en)
MX (1) MX3141E (en)
PL (3) PL92541B1 (en)
SU (4) SU533333A3 (en)

Also Published As

Publication number Publication date
ATA88775A (en) 1975-07-15
PL91890B1 (en) 1977-03-31
SU532338A3 (en) 1976-10-15
SU515443A3 (en) 1976-05-25
ES423974A1 (en) 1976-06-16
PL92541B1 (en) 1977-04-30
PL91891B1 (en) 1977-03-31
SU533333A3 (en) 1976-10-25
ES423975A1 (en) 1976-06-16
ES423973A1 (en) 1976-06-16
ES423976A1 (en) 1976-06-16
SU512696A3 (en) 1976-04-30

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