邻氯苯乙酸乙酯置于水,Sodium Hydroxide体系中,用 1,4-二氧六环 用作溶剂,化学反应 2.0H,以94%的收率获得邻氯苯乙酸 参考文献:Process For Synthesizing Phenylacetic Acid By Carbonylation Of Toluene 标题:Process For Synthesizing Phenylacetic Acid By Carbonylation Of Toluene 摘要:揭示了一种用于取代苯乙酸或其酯类似物的生产工艺.在这个工艺中,甲苯或带有各种取代基的甲苯,醇,氧化剂和一氧化碳被用作原料,通过过渡金属和配体形成的复合催化剂的催化作用,获得包含苯乙酸酯结构或其类似物的化合物,并且这些化合物被水解以获得各种基于取代苯乙酸的化合物.这类化合物及其衍生物在制药,农药,香水等行业中被广泛应用,作为重要的精细化学品.
专利号:US-8178474-B1 优先权日:1999-04-21 标题 :Functionalised solid support for alpha-oxoaldehyde synthesis 发明人:MELNYK OLEG; FRUCHART JEAN-SEBASTIEN; BOUREL LINE; GRAS-MASSE HELENE 权利人:MELNYK OLEG; FRUCHART JEAN-SEBASTIEN; BOUREL LINE; GRAS-MASSE HELENE; PASTEUR INSTITUT; CENTRE NAT RECH SCIENT 摘要:The invention relates to a functionalised solid support for the synthesis of compounds comprising at least one α-oxoaldehyde function, to a process for preparing it and to its applications, in particular for the preparation of a library of organic compounds, of a diagnostic reagent, of a microtitration plate and of a biochip, such as a DNA chip. The present invention also relates to a process for the synthesis of organic compounds comprising at least one α-oxoaldehyde function and to the α-oxoaldehyde peptides obtained using this process.
专利号:US-5354683-A 优先权日:1987-06-01 标题:Human immunodeficiency virus specific proteolytic enzyme and a method for its synthesis and renaturation 发明人:OROSZLAN STEPHEN; COPELAND TERRY D 权利人:US ARMY 摘要:HIV protease necessary for the natural synthesis of HIV has been identified and sequenced. This antibody cross reacts with the protease of HIV-2. In addition, a method for producing synthetic HIV-1 and HIV-2 protease having the correct stereospecific conformation and specific HIV proteolytic activity has been achieved. Assays for the synthetic proteases using synthetic peptide substrates have been developed.
专利号:US-6413957-B1 优先权日:1998-04-21 标题:Methods of inhibiting cell proliferation using indeno [1,2-c]pyrazol-4-ones 发明人:NUGIEL DAVID A; CARINI DAVID J; DI MEO SUSAN V; YUE EDDY W 权利人:BRISTOL MYERS SUIBB PHARMA COM 摘要:The present invention relates to the synthesis of a new class of indeno[1,2-c]pyrazol-4-ones of formula (I): n that are potent inhibitors of the class of enzymes known as cyclin dependent kinases, which relate to the catalytic subunits cdk1-7 and their regulatory subunits know as cyclins A-G. This invention also provides a novel method of treating cancer or other proliferative diseases by administering a therapeutically effective amount of one of these compounds or a pharmaceutically acceptable salt form thereof. Alternatively, one can treat cancer or other proliferative diseases by administering a therapeutically effective combination of one of the compounds of the present invention and one or more other known anti-cancer or anti-proliferative agents.
专利号:US-8188113-B2 优先权日:2006-09-14 标 题 :Dihydropyridopyrimidinyl, dihydronaphthyidinyl and related compounds useful as kinase inhibitors for the treatment of proliferative diseases 发明人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C 权利人:FLYNN DANIEL L; PETILLO PETER A; KAUFMAN MICHAEL D; PATT WILLIAM C; DECIPHERA PHARMACEUTICALS INC 摘要:The present invention relates to novel dihydropyridopyrimidinyl, dihydronaphthyridinyl, and related compounds which are kinase inhibitors and modulator useful for the treatment of various diseases. More particularly, the invention is concerned with such compounds, kinase/compound adducts, methods of treating diseases, and methods of synthesis of the compounds. Preferably, the compounds are useful for the modulation of kinase activity of Raf kinases and disease polymorphs thereof. Compounds of the present invention find utility in the treatment of mammalian cancers and especially human cancers including but not limited to malignant melanoma, colorectal cancer, ovarian cancer, papillary thyroid carcinoma, non small cell lung cancer, and mesothelioma. Compounds of the present invention also find utility in the treatment of rheumatoid arthritis and retinopathies including diabetic retinal neuropathy and macular degeneration.
专利号:WO-9700244-A1 优先权日:1995-06-19 标题 :Process for parallel synthesis of a non-peptide library 发明人:FRITZ JAMES E; KALDOR STEPHEN W 权利人:LILLY CO ELI; FRITZ JAMES E; KALDOR STEPHEN W 摘要:A process for the sequential preparation of a library of compounds having pharmaceutical usage. The process involves the sequential mixing of solution phase reagents, followed by scavenging of excess unreacted reagents with solid phase scavenging agents. The process is highly iterative and applicable for producing various ureas, thiureas, amides, carbonates and tertiary amines.
专利号:US-4426536-A 优先权日:1982-06-14 标 题:Synthesis of phenylacetic acid esters 发明人:ROBEY ROGER L 权利人:LILLY CO ELI 摘要:Esters of phenylacetic acids are prepared in a single step by hydrolysis of 2,2,2-trichloro-1-phenylethanes in inorganic basic media.
参考标题:An Approach To Spirooxindoles Via Palladium-Catalyzed Remote C-H Activation And Dual Alkylation With Ch2Br2 作者:Changdong Shao,Zhuo Wu,Xiaoming Ji,Bo Zhou,Yanghui Zhang 摘要:A Facile And Efficient Approach For The Synthesis Of Spirooxindoles Has Been Developed Via The Coupling Of Spirocyclic C, C-Palladacycles With Ch2Br2. The Key Spirocyclic Palladacycles Are Generated Catalytically Via Intramolecular Remote C-H Activation. A Range Of Spirooxindoles Can Be Synthesized In Good To Excellent Yields From Readily Available Starting Materials.
合成参考文献
摘要:Evano, G., Science of Synthesis, (2007) 20, 147. 摘要:Ziegler, T., Science of Synthesis, (2005) 21, 44.