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1. WO2020197042 - METHOD FOR PREPARING ROSUVASTATIN CALCIUM SALT

Publication Number WO/2020/197042
Publication Date 01.10.2020
International Application No. PCT/KR2019/017082
International Filing Date 05.12.2019
IPC
C07D 239/30 2006.01
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
239Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02not condensed with other rings
24having three or more double bonds between ring members or between ring members and non-ring members
28with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
30Halogen atoms or nitro radicals
A61K 31/505 2006.01
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
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
A61P 3/06 2006.01
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
06Antihyperlipidemics
CPC
A61K 31/505
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 ; or more; nitrogen atoms as the only ring heteroatoms, e.g. piperazine ; or tetrazines
505Pyrimidines; Hydrogenated pyrimidines, e.g. trimethoprim
A61P 3/06
AHUMAN NECESSITIES
61MEDICAL OR VETERINARY SCIENCE; HYGIENE
PSPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS OR MEDICINAL PREPARATIONS
3Drugs for disorders of the metabolism
06Antihyperlipidemics
C07B 2200/13
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
BGENERAL METHODS OF ORGANIC CHEMISTRY; APPARATUS THEREFOR
2200Indexing scheme relating to specific properties of organic compounds
13Crystalline forms, e.g. polymorphs
C07D 239/30
CCHEMISTRY; METALLURGY
07ORGANIC CHEMISTRY
DHETEROCYCLIC COMPOUNDS
239Heterocyclic compounds containing 1,3-diazine or hydrogenated 1,3-diazine rings
02not condensed with other rings
24having three or more double bonds between ring members or between ring members and non-ring members
28with hetero atoms or with carbon atoms having three bonds to hetero atoms with at the most one bond to halogen, directly attached to ring carbon atoms
30Halogen atoms or nitro radicals
Applicants
  • (주)헥사파마텍 HEXAPHARMATEC CO., LTD. [KR]/[KR]
Inventors
  • 한신 HAN, Shin
  • 이재형 LEE, Jae-Hyoung
  • 이경락 LEE, Gyung-Rak
Agents
  • 오국진 OH, Kook-Jin
Priority Data
10-2019-003414926.03.2019KR
Publication Language Korean (KO)
Filing Language Korean (KO)
Designated States
Title
(EN) METHOD FOR PREPARING ROSUVASTATIN CALCIUM SALT
(FR) PROCÉDÉ DE PRÉPARATION DE SEL DE ROSUVASTATINE CALCIQUE
(KO) 로수바스타틴 칼슘염의 제조방법
Abstract
(EN)
The present invention provides a novel intermediate useful for preparation of rosuvastatin calcium salt, that is, crystalline (E)-7-[4-(4-fluorophenyl)-6-isopropyl-2-[methyl(methylsulfonyl)amino]pyrimidin-5-yl]-(3R,5S)-3,5-dihydroxyhept-6-enoate(rosuvastatin) diisobutylamine salt. In addition, the present invention provides a method for preparing rosuvastatin calcium salt in a high chemical and optical purity by using the novel intermediate.
(FR)
La présente invention concerne un nouvel intermédiaire utile pour la préparation de sel de rosuvastatine calcique, à savoir, sel de (E)-7-[4-(4-fluorophényl)-6-isopropyl-2-[méthyl(méthylsulfonyl)amino]pyrimidin-5-yl]-(3R,5S)-3,5-dihydroxyhept-6-énoate(rosuvastatine) diisobutylamine cristallin. La présente invention concerne en outre un procédé de préparation d'un sel de rosuvastatine calcique ayant une pureté chimique élevée et une grande pureté optique à l'aide du nouvel intermédiaire.
(KO)
본 발명은 로수바스타틴 칼슘염의 제조에 유용한 신규의 중간체, 즉 결정성 (E)-7-[4-(4-플루오로페닐)-6-이소프로필-2-[메틸(메틸설포닐)아미노]피리미딘-5-일]-(3R,5S)-3,5-디히드록시헵트-6-엔산(로수바스타틴) 디이소부틸아민염을 제공한다. 또한, 본 발명은 상기 신규의 중간체를 사용하여 로수바스타틴 칼슘염을 높은 화학적 및 광학적 순도로 제조하는 방법을 제공한다.
Also published as
Latest bibliographic data on file with the International Bureau