4-溴吡啶置于盐酸,Palladium Diacetate,1,3-双(二苯基膦)丙烷,Potassium Carbonate体系中,用 水,N,N-二甲基甲酰胺 用作溶剂,化学反应 48.5H,反应生成4-乙酰吡啶 参考文献:Aqueous Dmf−potassium Carbonate As A Substitute For Thallium And Silver Additives In The Palladium-Catalyzed Conversion Of Aryl Bromides To Acetyl Arenes 标题:Aqueous Dmf−potassium Carbonate As A Substitute For Thallium And Silver Additives In The Palladium-Catalyzed Conversion Of Aryl Bromides To Acetyl Arenes 摘要:Highly Selective Palladium-Catalyzed Internal Alpha-Arylations Of Alkyl Vinyl Ethers With Aryl And Heteroaryl Bromides Were Conveniently Conducted In Aqueous Dmf With Potassium Carbonate As Base And With Dppp As Bidentate Ligand. The Corresponding Acetyl Arene Products Were,After Hydrolysis,Isolated In Good To Excellent Yields. This Heck Reaction Procedure Does Not Require Toxic Thallium Or Expensive Silver Salt Additives,Is Promoted By Water,And Is Suggested To Proceed Via Charged Organopalladium Intermediates. Single-Mode Microwave Irradiation Was Utilized In One Example To Shorten The Reaction Time. Doi:10.1021/jo015599F
专利号:US-5002641-A 优先权日:1990-06-28 标题:Electrochemical synthesis of niacin and other N-heterocyclic compounds 发明人:TOOMEY JR JOSEPH E 权利人:REILLY IND INC 摘要:An electrochemical oxidation of a pi-deficient N-heterocyclic precursor compound having an oxidizable organic group attached by a carbon-to-carbon linkage. This precursor compound is at least sparingly water soluble. The preferred electro-oxidation is conducted at an effective anode and in a medium which consists essentially of water, carboxylic acid, and the precursor compound. Preferred are electro-oxidations of substituted pyridine and quinoline bases and a particularly preferred aspect provides a convenient electrochemical synthesis of niacin from 3-methylpyridine.
专利号:US-2025129021-A1 优先权日:2023-09-19 标 题:Small molecule protein synthesis modulators 发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE 权利人:INTERDICT BIO INC 摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I), Formula (V)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
专利号:US-2025091989-A1 优先权日:2023-09-19 标 题 :Small molecule protein synthesis modulators 发明人:GYGI DAVID; BAHMANYAR SOGOLE SAMI; HAMANN LAWRENCE 权利人:INTERDICT BIO INC 摘要:The present disclosure provides compounds of the formulae herein (e.g., Formula (I)), and pharmaceutically acceptable salts thereof, which are useful for modulating protein synthesis (e.g., modulating synthesis of BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D). The present disclosure also provides pharmaceutical compositions and kits comprising the compounds, or pharmaceutically acceptable salts thereof, and methods of treating or preventing diseases or disorders (e.g., diseases or disorders associated with BCL-2, MYC, CCND1, MCL-1, ALK, KRAS-G12D) by administering to a subject in need thereof the compounds, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions thereof.
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-5663350-A 优先权日:1992-04-01 标题 :Process for the preparation of intermediates useful for the synthesis of histamine receptor antagonists 发明人:DURANT GRAHAM J; KHAN AMIN M 权利人:UNIV TOLEDO 摘要:The present invention relates to a novel process for the preparation of highly potent histamine receptor antagonists, in particular histamine H 3 -receptor antagonists. Also disclosed is a novel process for the preparation of intermediates useful in the preparation of histamine receptor antagonists, in particular H 3 -receptor antagonists.
专利号:US-8933237-B2 优先权日:2012-07-19 标 题:Methods for the synthesis of deuterated vinyl pyridine monomers 发明人:HONG KUNLUN; YANG JUN; BONNESEN PETER V 权利人:UT BATTELLE LLC 摘要:Methods for synthesizing deuterated vinylpyridine compounds of the Formula (1), wherein the method includes: (i) deuterating an acyl pyridine of the Formula (2) in the presence of a metal catalyst and D 2 O, wherein the metal catalyst is active for hydrogen exchange in water, to produce a deuterated acyl compound of Formula (3); (ii) reducing the compound of Formula (3) with a deuterated reducing agent to convert the acyl group to an alcohol group, and (iii) dehydrating the compound produced in step (ii) with a dehydrating agent to afford the vinylpyridine compound of Formula (1). The resulting deuterated vinylpyridine compounds are also described.
[参考文献]: Anita Toulmin, Et Al. Toward Prediction Of Alkane/water Partition Coefficients. J Med Chem. 2008 Jul 10;51(13):3720-30. [参考文献]: G M Abu El-Reash, Et Al. Characterization And Biological Studies On Co(Ii), Ni(Ii) And Cu(Ii) Complexes Of Carbohydrazones Ending By Pyridyl Ring. Spectrochim Acta A Mol Biomol Spectrosc. 2013 Mar:104:26-34. [参考文献]: Gordana M Raki, Et Al. Novel Trans-Dichloridoplatinum(Ii) Complexes With 3- And 4-Acetylpyridine: Synthesis, Characterization, Dft Calculations And Cytotoxicity. Eur J Med Chem. 2009 May;44(5):1921-5. [参考文献]: H Beraldo, Et Al. Spectral Studies Of Semicarbazones Derived From 3- And 4-Formylpyridine And 3- And 4-Acetylpyridine: Crystal And Molecular Structure Of 3-Formylpyridine Semicarbazone. Spectrochim Acta A Mol Biomol Spectrosc. 2001 Aug;57(9):1847-54. [参考文献]: Koji Uwai, Et Al. Purification And Characterization Of Rat Liver Enzyme Catalyzing Stereoselective Reduction Of Acetylpyridines. Chirality. 2005 Oct;17(8):494-500.
合成参考文献
摘要:Götzinger, A. C.; Müller, T. J. J., Science of Synthesis Knowledge Updates, (2017) 3, 127. 摘要:Singh, F. V., Science of Synthesis Knowledge Updates, (2021) 1, 154. 摘要:Sharma, U.; Kumar, R.; Gupta, S. S.; Chandra, D., Science of Synthesis Knowledge Updates, (2022) 2, 146. 摘要:Glushkov, V. A.; Shklyaev, Yu. V., Science of Synthesis Knowledge Updates, (2018) 3, 240. 摘要:Spitzner, D., Science of Synthesis Knowledge Updates, (2016) 1, 336.