专利号:US-6800785-B1 优先权日:2002-10-15 标题:Process for the synthesis of estrogen receptor modulators 发明人:MENG DONGFANG 权利人:MERCK & CO INC 摘要:The present invention relates to processes for the synthesis of intermediates useful for the synthesis of estrogen receptor modulators. The process includes new methods for annelating 5-, 6- and 7-membered cycloalkenones onto an indanone.
专利号:US-2007293706-A1 优先权日:2004-11-01 标 题:Synthesis Of 1,5-Disubstituted-2-Hydroxy-Gibbatetraen-6-Ones 发明人:WILKENING ROBERT R; FRIED AMY; PARKER DANN L JR 权利人:WILKENING ROBERT R; FRIED AMY; PARKER DANN L JR 摘要:1,5-disubstituted-2-hydroxy-gibbatetraen-6-ones are useful as estrogen receptor modulators and as precursors to estrogen receptor modulators. The current invention provides a method for the synthesis of 1,5-disubstituted-2-hydroxy-gibbatetraen-6-ones from simple indanone starting materials via a Robinson-type annulation followed by an internal alkylation reaction. This invention further describes the novel use of a fluoroethyl substituent as a latent alkylating group for an internal cyclization reaction.
专利号:WO-2015131100-A1 优先权日:2014-02-28 标题:Ligand-controlled c(sp3)-h arylation and olefination in synthesis of unnatural chiral alpha amino acids 发明人:YU JIN-QUAN 权利人:SCRIPPS RESEARCH INST 摘要:The use of ligands to tune the reactivity and selectivity of transition metal-catalysts for C(-sp3)-H bond functionalization is a central challenge in synthetic organic chemistry. Herein, we report a rare example of catalyst-controlled C(sp3)-H arylation using pyridine and quinoline derivatives: the former promotes exclusive monoarylation, whereas the latter activates the catalyst further to achieve diarylation. Successive application of these ligands enables the sequential diarylation of a methyl group in an alanine derivative with two different aryl iodides, affording a wide range of β-Ar-p-Ar ' -cc-amino acids with excellent levels of diastereoselectivity (d.r. > 20:1). Both configurations of the β-chiral center can be accessed by choosing the order in which the aryl groups are installed. The use of a quinoline derivative as a ligand also enables C(sp3)-H olefination of a protected alanine.
专利号:US-8633182-B2 优先权日:2012-05-30 标题:Indanyloxyphenylcyclopropanecarboxylic acids 发明人:HAMPRECHT DIETER; FRATTINI SARA; LINGARD IAIN; PETERS STEFAN 权利人:HAMPRECHT DIETER; FRATTINI SARA; LINGARD IAIN; PETERS STEFAN; BOEHRINGER INGELHEIM INT 摘要:The present invention relates to compounds of general formula I, n nwherein the groups R 1 , R 2 , R 3 , m and n are defined as in claim 1 , which have valuable pharmacological properties, in particular bind to the GPR40 receptor and modulate its activity. The compounds are suitable for treatment and prevention of diseases which can be influenced by this receptor, such as metabolic diseases, in particular diabetes type 2. Furthermore, the invention relates to novel intermediates, useful for the synthesis of compounds of formula I.
专利号:US-2023002426-A1 优先权日:2019-11-15 标题 :Chiral synthesis of a tertiary alcohol
专利号:AU-2005302235-A1 优先权日:2004-11-01 标 题 :Synthesis of 1,5-disubstituted-2-hydroxy-gibbatetraen-6-ones
[参考文献]: Tiffany J Somers-Edgar, Et Al. Coenzyme Q0 Induces Apoptosis And Modulates The Cell Cycle In Estrogen Receptor Negative Breast Cancer Cells. Anticancer Drugs. 2009 Jan;20(1):33-40.
合成参考文献
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