PREPARATION METHOD FOR (3R,5R)-7-[2-(4-FLUROPHENYL)-5-ISOPROPYL-3-PHENYL-4-[(4-HYDROXYMETHYLPHENYLAMINO)CARBONYL]-PYRRROL-1-YL]-3,5-DIHYDROXY HEPTANOIC ACID HEMICALCIUM SALT, INTERMEDIATE USED THEREFOR, AND PREPARATION METHOD FOR INTERMEDIATE

• Main Authors: SOHN, Se-Il, LEE, Won-Il, PARK, Sang-Wook, KIM, Churl-Woo, CHO, Min-Yong, JEONG, Seo-Hee, PARK, Eun-Jung, KIM, Bo-Jung, SHIN, Sang-Yun
• Format: Patent
• Language: English; French; Korean
• Published: 27.02.2020
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; CHEMISTRY; HETEROCYCLIC COMPOUNDS; METALLURGY; ORGANIC CHEMISTRY

The present invention provides: a preparation method for a (3R,5R)-7-[2-(4-flurophenyl)-5-isopropyl-3-phenyl-4-[(4-hydroxymethylphenylamino)carbonyl]-pyrrrol-1-yl]-3,5-dihydroxy heptanoic acid hemicalcium salt; an intermediate used therefor; and a preparation method for the intermediate. The preparation method of the present invention is performed in a convergent synthesis manner in which main structure portions of the (3R,5R)-7-[2-(4-flurophenyl)-5-isopropyl-3-phenyl-4-[(4-hydroxymethylphenylamino)carbonyl]-pyrrrol-1-yl]-3,5-dihydroxy heptanoic acid hemicalcium salt are separately synthesized, and then coupled. Therefore, related substances can be easily controlled and the preparation time can be shortened, leading to an improvement in productivity of compounds as well as an increase in yield of a final compound. La présente invention concerne : un procédé de préparation de sel hemicalcique de l'acide (3R,5R)-7-[2-(4-flurophényl)-5-isopropyl-3-phényl-4-[(4-hydroxyméthylphénylamino)carbonyl]-pyrrrol-1-yl]-3,5-dihydroxyheptanoïque ; un intermédiaire utilisé à cet effet ; et un procédé de préparation de l'intermédiaire Le procédé de préparation selon la présente invention est réalisé d'une manière à synthèse convergente, des parties de structure principale du sel hemicalcique de l'acide (3R,5R)-7-[2-(4-flurophényl)-5-isopropyl-3-phényl-4-[(4-hydroxyméthylphénylamino)carbonyl]-pyrrrol-1-yl]-3,5-dihydroxyheptanoïque étant synthétisés séparément, puis couplés. Par conséquent, des substances apparentées peuvent être facilement contrôlées et le temps de préparation peut être raccourci, conduisant à une amélioration de la productivité des composés ainsi qu'à une augmentation du rendement du composé final. 본 발명은 (3R,5R)-7-(2-(4-플루오로페닐)-5-이소프로필-3-페닐-4-((4-히드록시 메틸 페닐 아미노)카보닐)-피롤-1-일)-3,5-디히드록시 헵탄산 헤미칼슘염의 제조방법, 이에 사용되는 중간체 및 이의 제조방법을 제공한다. 본 발명의 제조방법은, (3R,5R)-7-[2-(4-플루오로페닐)-5-이소프로필-3-페닐-4-[(4-히드록시메틸페닐아미노)카보닐]-피롤-1-일]-3,5-디히드록시 헵탄산 헤미칼슘염의 주요 구조부들 각각을 개별적으로 합성한 후 커플링 하는 수렴합성 방식으로 수행된다. 이에 따라, 유연물질을 용이하게 제어하고 제조시간을 단축시킬 수 있어 화합물의 생산성을 향상시킬 수 있고, 최종 화합물의 수율 또한 높일 수 있다.