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1. WO2000043350 - CRYSTAL POLYMORPHISM OF AMINOETHYLPHENOXYACETIC ACID DERIVATIVE

Publication Number WO/2000/043350
Publication Date 27.07.2000
International Application No. PCT/JP2000/000168
International Filing Date 17.01.2000
Chapter 2 Demand Filed 18.07.2000
IPC
C07C 213/10 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
213Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
10Separation; Purification; Stabilisation; Use of additives
C07C 217/60 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
217Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
54having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
56with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by singly-bound oxygen atoms
60linked by carbon chains having two carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
CPC
A61P 13/04
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
04for urolithiasis
A61P 13/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
13Drugs for disorders of the urinary system
06Anti-spasmodics
C07C 213/10
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
213Preparation of compounds containing amino and hydroxy, amino and etherified hydroxy or amino and esterified hydroxy groups bound to the same carbon skeleton
10Separation; Purification; Stabilisation; Use of additives
C07C 217/60
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
CACYCLIC OR CARBOCYCLIC COMPOUNDS
217Compounds containing amino and etherified hydroxy groups bound to the same carbon skeleton
54having etherified hydroxy groups bound to carbon atoms of at least one six-membered aromatic ring and amino groups bound to acyclic carbon atoms or to carbon atoms of rings other than six-membered aromatic rings of the same carbon skeleton
56with amino groups linked to the six-membered aromatic ring, or to the condensed ring system containing that ring, by carbon chains not further substituted by singly-bound oxygen atoms
60linked by carbon chains having two carbon atoms between the amino groups and the six-membered aromatic ring or the condensed ring system containing that ring
Applicants
  • KISSEI PHARMACEUTICAL CO., LTD. [JP/JP]; 19-48, Yoshino Matsumoto-shi Nagano 399-8710, JP (AllExceptUS)
  • TODA, Michio [JP/JP]; JP (UsOnly)
  • TAMAI, Tetsuro [JP/JP]; JP (UsOnly)
  • TANAKA, Nobuyuki [JP/JP]; JP (UsOnly)
  • KASAI, Kiyoshi [JP/JP]; JP (UsOnly)
  • SONEHARA, Junichi [JP/JP]; JP (UsOnly)
  • TSURU, Eiji [JP/JP]; JP (UsOnly)
Inventors
  • TODA, Michio; JP
  • TAMAI, Tetsuro; JP
  • TANAKA, Nobuyuki; JP
  • KASAI, Kiyoshi; JP
  • SONEHARA, Junichi; JP
  • TSURU, Eiji; JP
Priority Data
11/1363921.01.1999JP
Publication Language Japanese (JA)
Filing Language Japanese (JA)
Designated States
Title
(EN) CRYSTAL POLYMORPHISM OF AMINOETHYLPHENOXYACETIC ACID DERIVATIVE
(FR) POLYMORPHISME CRISTALLIN DE DERIVE D'ACIDE AMINOETHYLPHENOXYACETIQUE
Abstract
(EN)
Crystal polymorphism of 2-[4-[2-[[1s,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methyl ethyl]amino]ethyl]phenoxy]acetic acid which has potent $g(b)2 adrenergic receptor stimulating and $g(b)3-adrenergic receptor stimulating effects, is useful in relieving a pain, promoting calculi removal, etc. in urinary lithiasis and shows intense diffraction peaks at 10.8, 19.1, 19.3, 19.8, 20.6 and 27.0° in the powder x-ray diffractometry pattern at a diffraction angle (2/$g(u)0±0.1). It is produced by, for example, hydrolyzing ethyl 2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphenyl)-1-methylethyl]amino]ethy]phenoxy]acetate phosphate by using sodium hydroxide, adding an aqueous solution of phosphoric acid at 40°C or above to give the above compound, adding a solvent mixture comprising methanol with water or methanol and then stirring in a suspended state at from 40°C to the reflux point for 30 minutes to several hours.
(FR)
L'invention concerne un polymorphisme cristallin d'acide 2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphényle)-1-méthyléthyl]amino]éthyl]phénoxy]acétique ayant de puissants effets de stimulation du récepteur $g(b)2-adrénergique et du récepteur $g(b)3-adrénergique, utile pour soulager la douleur, favoriser l'élimination des calculs, etc., dans la lithiase urinaire, avec des crêtes de diffraction intense à 10,8, 19,1, 19,3, 19,8, 20,6 et 27° dans le diagramme du diffractomètre de rayons X sur poudre, à un angle de diffraction (2$g(u)±0,1). Il est possible d'obtenir ce produit, par exemple, en effectuant l'hydrolyse d'éthyle 2-[4-[2-[[1S,2R]-2-hydroxy-2-(4-hydroxyphényle)-1- méthyléthyl]amino]éthyl]phénoxy]acétate phosphate : à cet effet, on utilise de l'hydroxyde de sodium auquel il faut ajouter une solution aqueuse d'acide phosphorique à 40° C ou plus pour donner le composé susmentionné, avec adjonction d'un mélange solvant comprenant du méthanol et de l'eau, puis mélange en suspension à partir de 40° C jusqu'au point de reflux pendant une durée comprise entre 30 minutes et plusieurs heures.
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