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更新于：2025-05-07

Panomifene

帕诺米芬

更新于：2025-05-07

概要

基本信息

药物类型

小分子化药

别名

+ [1]

靶点

作用方式

拮抗剂

作用机制

ERs拮抗剂(雌激素受体家族拮抗剂)

治疗领域

肿瘤皮肤和肌肉骨骼疾病

在研适应症-

非在研适应症

乳腺癌

原研机构

IVAX LLC

在研机构-

非在研机构

Egis Gyógyszergyár Zrt.

IVAX LLC

权益机构-

最高研发阶段终止临床2期

首次获批日期-

最高研发阶段(中国)-

特殊审评-

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结构/序列

分子式C25H24F3NO2

InChIKeyMHXVDXXARZCVRK-WCWDXBQESA-N

CAS号77599-17-8

关联

100 项与帕诺米芬相关的临床结果

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100 项与帕诺米芬相关的转化医学

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100 项与帕诺米芬相关的专利（医药）

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项与帕诺米芬相关的文献（医药）

2005-09-01·Tetrahedron

Highly regio- and stereo-selective carbometallation reaction of fluorine-containing internal acetylenes with organocopper reagents

作者: Takashi Ishihara ; Jungha Chae ; Atsushi Noiri ; Takeshi Daitoh ; Tsutomu Konno ; Hiroki Yamanaka

The carbometalation reactions of fluoroalkylated internal alkynes with various organocopper reagents derived from organolithium, Grignard, and organozinc reagents were examinedAll carbocupration reactions proceeded smoothly in a highly regio- and stereoselective manner to give the vinylcopper intermediates.The intermediates reacted with H⁺ smoothly, leading to trisubstituted alkenes in high to excellent yields, whereas they reacted only with strictly limited carbon electrophiles such as allyl, crotyl, methallyl bromide, probably due to the low reactivity exerted by an electron-withdrawing fluoroalkyl group.Treatment of vinylcopper with iodine resulted in a high yield of the vinyl iodide, which was employed successfully for Suzuki-Miyaura and Sonogashira cross-coupling reactions.In addition, two key reactions, the carbocupration and the Suzuki-Miyaura cross-coupling reaction realized the first highly stereoselective total synthesis of anti-estrogen drug, panomifene.

2005-07-21·ACS Symposium Series

A New Aspect of Fluoroalkylated Acetylenes: Synthesis and Applications—Hydrometallation and Carbometallation

作者: Ishihara, Takashi ; Konno, Tsutomu

A review in which the facile and practical syntheses of various F-containing alkynes are described.Thus-obtained alkynes undergo smooth hydrostannation, hydroboration, carbostannylation, and carbocupration reactions to afford the corresponding hydro- and carbometalated adducts in a highly regio- and stereoselective manner.With this synthetic methodol., a short total synthesis of estrogen-dependent antitumor agent, panomifene was realized.

2005-05-01·Tetrahedron Letters

A highly stereoselective preparation of CF3-substituted 1-aryl-1,2-diphenylethenes: application to the synthesis of panomifene

作者: Kim, Myong Sang ; Jeong, In Howa

β-CF₃-α,β-diphenylvinyl sulfide I (R = SPh) was prepared stereoselectively in 77% yield from the reaction of fluoride II with phenyllithium at room temperature for 5 h.Oxidation of I (R = SPh) with MCPBA afforded the corresponding vinyl sulfone I (R = SO₂) as a pure trans-isomer after crystallization in a mixture of CH₂Cl₂ and hexane.The addition-elimination reaction of this sulfone with substituted phenyllithium compounds provided triarylethenes, such as III, in 51-82% yields stereospecifically.Similarly, the treatment of the sulfone with p-(2-chloroethoxy)phenyllithium in the presence of 12-crown-4 (20 mol %) at -10 °C, followed by slowly warming to room temperature, resulted in the formation of the corresponding panomifene precursor IV in 82% yield, which was reacted with 2-aminoethanol to give panomifene in 82% yield.

100 项与帕诺米芬相关的药物交易

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