PROCESS FOR PREPARATION OF SELECTIVE ESTROGEN RECEPTOR DECOMPOSER

PROCESS FOR PREPARATION OF SELECTIVE ESTROGEN RECEPTOR DECOMPOSER

To provide a selective estrogen receptor decomposer (SERD) as well as an intermediate thereof and a salt thereof including pharmaceutically acceptable salt, and a method for making a pharmaceutical composition thereof.SOLUTION: Disclosed is a method for producing a compound of formula A [in the form...

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Hauptverfasser: MAI KHANH NGUYEN HAWK, NICHOLAS ANDREW MAGNUS, BORIS ARNOLDOVICH CZESKIS, DOUGLAS PATTON KJELL, ALONSO JOSE ARGUELLES DELGADO, LU YU, DAVID MICHAEL REMICK
Format: Patent
Sprache:eng ; jpn
Schlagworte:
CHEMISTRY
HETEROCYCLIC COMPOUNDS
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
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Zusammenfassung:To provide a selective estrogen receptor decomposer (SERD) as well as an intermediate thereof and a salt thereof including pharmaceutically acceptable salt, and a method for making a pharmaceutical composition thereof.SOLUTION: Disclosed is a method for producing a compound of formula A [in the formula, either R1 or R2 is independently Cl, F, -CF3 or -CH3 and the other is H, R7 is H or PG, and PG is an alcohol protecting group.] having an enantiomeric excess percentage of at least about 92%.SELECTED DRAWING: None 【課題】選択的エストロゲン受容体分解剤（ＳＥＲＤ）、並びにそれらの中間体、薬学的に許容される塩を含むそれらの塩、及びそれらの薬学的組成物を作製する方法を提供する。【解決手段】少なくとも約９２％のエナンチオマー過剰率を有する式Ａの化合物TIFF2023162334000159.tif3774［式中、Ｒ１又はＲ２のいずれかが、独立して、Ｃｌ、Ｆ、－ＣＦ３又は－ＣＨ３であり、他方が、Ｈであり、Ｒ７が、Ｈ又はＰＧであり、ＰＧが、アルコール保護基である。］を製造する方法が開示される。【選択図】なし