专利号:US-7652137-B2 优先权日:2003-03-06 标 题:Synthesis of 5 substituted 7-azaindoles and 7-azaindolines 发明人:GRACZYK PIOTR PAWEL; KHAN AFZAL; BHATIA GURPREET SINGH 权利人:EISAI R&D MAN CO LTD 摘要:The present invention provides a novel substituted azaindoline intermediate of formula (I) and a method for its synthesis. The novel substitued azaindoline intermediate (I) is provided for use in the manufacture of 5-substituted 7-azaindolines and 5-substituted 7-azaindoles.
专利号:US-5098602-A 优先权日:1988-05-11 标题 :Novel halogen-containing ester compounds, and their intermediates, and method of producing the same as well as liquid crystal compositions containing the same and light switching elements 发明人:HIRAI TOSHIHIRO; YOSHIZAWA ATSUSHI; NISHIYAMA ISA; FUKUMASA MITSUO; SHIRATORI NOBUYUKI; YOKOYAMA AKIHISA 权利人:NIPPON MINING CO 摘要:This invention provides a novel halogen-containing ester compound represented by the following general formula (I): ##STR1## (wherein R is an alkyl group, A is selected from a single bond, --O--, --COO-- and --CO--, both of X and Y are halogen atoms or either one of X and Y is a halogen atom and the other is a hydrogen atom, each of m and n is 0 or 1, m+n=0 or 1, each of k and l is an integer of 1 or more, provide k 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-8399680-B2 优先权日:2007-09-28 标 题:Arylamine synthesis method 发明人:TAILLEFER MARC; XIA NING 权利人:TAILLEFER MARC; XIA NING; CENTRE NAT RECH SCIENT 摘要:The invention relates to a method for preparing arylamines and, in particular, a method for preparing aniline and anilines substituted on the aromatic ring from ammonia, under easily-industrialized mild conditions with good selectivity and yields, in the presence of a catalytic system including a copper complex.
专利号:US-7615634-B2 优先权日:2003-02-10 标题:4-aminopyrimidine-5-one derivatives 发明人:BARTKOVITZ DAVID JOSEPH; CHU XIN-JIE; DING QINGJIE; JIANG NAN; LOVEY ALLEN JOHN; MOLITERNI JOHN ANTHONY; MULLIN JR JOHN GUILFOYLE; VU BINH THANH; WOVKULICH PETER MICHAEL 权利人:HOFFMANN LA ROCHE 摘要:Novel intermediate compounds are disclosed. These compounds are useful in the synthesis of 4-aminopyrimidine-5-one derivatives that inhibit cyclin-dependent kinases, in particular cyclin-dependent kinase 4 (Cdk4). The 4-aminopyrimidine-5-one derivatives and their pharmaceutically acceptable salts have antiproliferative activity and are useful in the treatment or control of cancer, in particular solid tumors.
专利号:CN-113087691-B 优先权日:2021-03-26 标题:A method for the synthesis of chiral aryl tertiary alcohols and benzopyrans based on a kinetic resolution strategy
[参考文献]: Pierre-Yves Michellys, Et Al. Design, Synthesis And Structure-Activity Relationship Of Novel Rxr-Selective Modulators. Bioorg Med Chem Lett. 2004 Mar 22;14(6):1593-8.
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