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1. WO2012165547 - METHOD FOR MANUFACTURING PYRAZOLE DERIVATIVE

Publication Number WO/2012/165547
Publication Date 06.12.2012
International Application No. PCT/JP2012/064075
International Filing Date 31.05.2012
IPC
C07D 231/38 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
231Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
02not condensed with other rings
10having two or three double bonds between ring members or between ring members and non-ring members
14with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
38Nitrogen atoms
A61K 31/496 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
KPREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES
31Medicinal preparations containing organic active ingredients
33Heterocyclic compounds
395having nitrogen as a ring hetero atom, e.g. guanethidine or rifamycins
495having six-membered rings with two nitrogen atoms as the only ring hetero atoms, e.g. piperazine
496Non-condensed piperazines containing further heterocyclic rings, e.g. rifampin, thiothixene
A61P 3/10 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
08for glucose homeostasis
10for hyperglycaemia, e.g. antidiabetics
A61P 43/00 2006.1
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/-A61P41/108
C07D 417/14 2006.1
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
417Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/196
14containing three or more hetero rings
CPC
A61P 3/10
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
08for glucose homeostasis
10for hyperglycaemia, e.g. antidiabetics
A61P 43/00
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
43Drugs for specific purposes, not provided for in groups A61P1/00-A61P41/00
C07D 231/38
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
231Heterocyclic compounds containing 1,2-diazole or hydrogenated 1,2-diazole rings
02not condensed with other rings
10having two or three double bonds between ring members or between ring members and non-ring members
14with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, e.g. ester or nitrile radicals, directly attached to ring carbon atoms
38Nitrogen atoms
C07D 417/14
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
417Heterocyclic compounds containing two or more hetero rings, at least one ring having nitrogen and sulfur atoms as the only ring hetero atoms, not provided for by group C07D415/00
14containing three or more hetero rings
Applicants
  • 田辺三菱製薬株式会社 MITSUBISHI TANABE PHARMA CORPORATION [JP]/[JP] (AllExceptUS)
  • 赤星 文彦 AKAHOSHI, Fumihiko [JP]/[JP] (UsOnly)
  • 桐原 伸治 KIRIHARA, Shinji [JP]/[JP] (UsOnly)
Inventors
  • 赤星 文彦 AKAHOSHI, Fumihiko
  • 桐原 伸治 KIRIHARA, Shinji
Agents
  • 高島 一 TAKASHIMA, Hajime
Priority Data
2011-12381901.06.2011JP
Publication Language Japanese (ja)
Filing Language Japanese (JA)
Designated States
Title
(EN) METHOD FOR MANUFACTURING PYRAZOLE DERIVATIVE
(FR) PROCÉDÉ DE FABRICATION D'UN DÉRIVÉ DE PYRAZOLE
(JA) ピラゾール誘導体の製造方法
Abstract
(EN) The present invention provides a prolinamide compound useful as a drug or the like and an industrially advantageous method for producing a piperazinyl pyrazole compound that is a production intermediate of the prolinamide compound. Specifically, the invention is a method for producing a compound represented by general formula (1) as represented by the following formula (where the symbols in the formula are the same as defined in the specification) or a salt thereof, wherein a compound represented by general formula (2) is produced, a pyrazole ring being formed via a reaction between a compound represented by general formula (3) and phosphorus pentasulfide; and, once the compound represented by general formula (2) is deprotected, a carboxylate of a compound represented by general formula (6) is produced, the compound obtained by forming a carboxylic acid and a salt.
(FR) La présente invention concerne un composé prolinamide utile comme un médicament ou similaire et un procédé industriellement avantageux pour fabriquer un composé pipérazinyl pyrazole qui est un intermédiaire de fabrication du composé polinamide. De façon spécifique, l'invention consiste en un procédé pour la production d'un composé représenté par la formule générale (1) telle que représentée par la formule suivante (où les symboles dans la formule sont les mêmes que ceux définis dans la description) ou un sel de celui-ci, dans lequel un composé représenté par la formule générale (2) est produit, un noyau pyrazole étant formé par l'intermédiaire d'une réaction entre un composé représenté par la formule générale (3) et le pentasulfure de phosphore ; et, une fois que le composé représenté par la formule générale (2) est déprotégé, un carboxylate d'un composé représenté par la formule générale (6) est produit, le composé obtenu par formation d'un acide carboxylique et un sel.
(JA)  本発明は、医薬等として有用なプロリンアミド化合物、及びその製造中間体であるピペラジニルピラゾール化合物の工業的に有利な製造方法を提供する。すなわち、本発明は、以下の式:(式中の各記号は、明細書中の定義と同義である)で表される一般式(1)で表される化合物、又はその塩の製造方法であって、一般式(3)で表される化合物と五硫化リンとの反応によりピラゾール環を形成させる一般式(2)で表される化合物の製造、並びに一般式(2)で表される化合物を脱保護後、カルボン酸と塩形成させてなる一般式(6)で表される化合物のカルボン酸塩の製造を経由する、製造方法である。
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