PROCESSES FOR PREPARATION OF LATANOPROSTENE BUNOD AND INTERMEDIATE THEREOF, AND COMPOSITIONS COMPRISING THE SAME

• Main Authors: WEI TZYH-MANN, WEI SHIH-YI, HSU MING KUN
• Format: Patent
• Language: English; Japanese
• Published: 03.02.2022
• Subjects: ACYCLIC OR CARBOCYCLIC COMPOUNDS; ACYCLIC, CARBOCYCLIC OR HETEROCYCLIC COMPOUNDS CONTAININGELEMENTS OTHER THAN CARBON, HYDROGEN, HALOGEN, OXYGEN, NITROGEN,SULFUR, SELENIUM OR TELLURIUM; CHEMISTRY; HUMAN NECESSITIES; HYGIENE; MEDICAL OR VETERINARY SCIENCE; METALLURGY; ORGANIC CHEMISTRY; PREPARATIONS FOR MEDICAL, DENTAL, OR TOILET PURPOSES; SPECIFIC THERAPEUTIC ACTIVITY OF CHEMICAL COMPOUNDS ORMEDICINAL PREPARATIONS

To provide: processes for preparing latanoprostene bunod and an intermediate prepared from the process; and latanoprostene bunod compositions having high-purity latanoprostene bunod.SOLUTION: A process for preparing latanoprostene bunod comprises reacting latanoprost acid with 1,4-butanediol dinitrate. Preferably, the preparing process includes a process for purification of crude latanoprostene bunod by silylating all hydroxyl groups in the crude latanoprostene bunod with a silylating agent comprising a residue -SiRaRbRc so as to form a compound of formula LB-3Si.SELECTED DRAWING: None 【課題】ラタノプロステン・ブノドの調製方法及び該方法で調製された中間体、また、高純度のラタノプロステン・ブノドを含む、ラタノプロステン・ブノド組成物を提供する。【解決手段】ラタノプロスト酸を１，４－ブタンジオール・ジニトラートと反応させる、ラタノプロステン・ブノドの製造方法である。好ましくは、粗ラタノプロステン・ブノド中の全ヒドロキシ基を－ＳｉＲaＲbＲc残基を含むシリル化剤でシリル化して下式ＬＢ－３Ｓｉで示される化合物を形成することによる、粗ラタノプロステン・ブノドの精製方法を含む、製造方法である。TIFF2022022148000015.tif57170【選択図】なし