3,4-Dimethoxyacetophenone Semicarbazone置于1-Benzyl-4-Aza-1-Azoniabiyclo<2.2.2>octane Peroxodisulfate体系中,用 乙腈 用作溶剂,化学反应 1.33H,以59%的收率获得3,4-二甲氧基苯乙酮 参考文献:Bis(1-Benzyl-4-Aza-1-Azoniabicyclo[2.2.2]octane) Peroxodisulfate: A Mild And Efficient Oxidant For Cleavage Of Nitrogen Double Bonds And Oxidation Of Alcohols Under Anhydrous Conditions 标题:Bis(1-Benzyl-4-Aza-1-Azoniabicyclo[2.2.2]octane) Peroxodisulfate: A Mild And Efficient Oxidant For Cleavage Of Nitrogen Double Bonds And Oxidation Of Alcohols Under Anhydrous Conditions 摘要:双(1-苄基-4-氮杂-1-氮鎓双环[2.2.2]辛烷)过氧二硫酸酯(1),可方便地由市售的1,4-二氮双环[2.2.2]辛烷和过氧二硫酸钾制备成橙色固体.该试剂能轻易地将脲,缩氨基脲,肟和醇转化为相应的羰基化合物,且产率极佳. Doi:10.1246/bcsj.71.2655
专利号:US-10308588-B2 优先权日:2014-12-15 标 题 :Synthesis of amides and amines from aldehydes or ketones by heterogeneous metal catalysis 发明人:CÓRDOVA ARMANDO; PALO-NIETO CARLOS; AFEWERKI SAMSON 权利人:ORGANOFUEL SWEDEN AB 摘要:A mild and efficient synthesis of primary amines and amides from aldehydes or ketones using a heterogeneous metal catalyst and amine donor is disclosed. The initial heterogeneous metal-catalyzed reaction between the carbonyl and the amine donor components is followed by the addition of a suitable acylating agent component in one-pot, thus providing a catalytic one-pot three-component synthesis of amides. Integration of enzyme catalysis allows for eco-friendly one-pot co-catalytic synthesis of amides from aldehyde and ketone substrates, respectively. The process can be applied to asymmetric synthesis or to the co-catalytic one-pot three-component synthesis of capsaicin and its analogues from vanillin or vanillyl alcohol. A co-catalytic reductive amination/dynamic kinetic resolution (dkr) relay sequence for the asymmetric synthesis of optically active amides from ketones is disclosed. Implementation of a catalytic reductive amination/kinetic resolution (kr) relay sequence produces the corresponding optically active amide product and optical active primary amine product with the opposite stereochemistry from the starting ketones.
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-4490374-A 优先权日:1982-09-30 标 题:5,6-Dialkoxy-3,4-optionally substituted-2(1H)quinazolinones, composition and method of use 发明人:BANDURCO VICTOR T; LEVINE SEYMOUR D; MULVEY DENNIS M; TOBIA ALFONSO J 权利人:ORTHO PHARMA CORP 摘要:The synthesis of substituted quinazolinones is described. The novel quinazolinones are renal vasodilators and thereby increase renal blood flow, and are useful as cardiovascular agents.
专利号:WO-2024003151-A1 优先权日:2022-06-28 标 题:Chemical synthesis platform 发明人:CRONIN LEROY 权利人:UNIV GLASGOW COURT 摘要:The invention relates to a method for generating a database for chemical syntheses and a method for performing a chemical synthesis using a database. The method for generating a database comprises generating a series of instruction sets for a series of chemical syntheses from the literature, wherein each instruction set is a machine readable and executable universal language for a chemical synthesiser; assembling the series of instructions sets within a database, and making the instruction sets available for access and autonomous execution by a chemical synthesiser. The method for performing a chemical synthesis comprises accessing an instruction set from a database, providing the instruction set to a chemical synthesiser, and autonomously executing the instruction set on the chemical synthesiser thereby to perform the chemical synthesis. The invention makes use of a standardised and step-focussed syntax to describe the chemical syntheses, and a universal synthesis automation platform.
专利号:US-7250435-B2 优先权日:1999-10-20 标 题:Acylsemicarbazides as cyclin dependent kinase inhibitors useful as anti-cancer and anti-proliferative agents 发明人:NUGIEL DAVID A; CARINI DAVID J; DI MEO SUSAN V; VIDWANS ANUP P; YUE EDDY 权利人:BRISTOL MYERS SQUIBB PHARMA CO 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 nthat 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.n n 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-5126351-A 优先权日:1991-01-24 标 题:Antitumor compounds 发明人:LUZZIO MICHAEL J; BESTERMAN JEFFREY M; EVANS MICHAEL G; JOHNSON M ROSS 权利人:GLAXO INC 摘要:The present invention relates to the compounds of formula (I), ##STR1## wherein: R 1 is hydrogen, hydroxy or amino; n R 2 is hydrogen, hydroxy, methoxy or methoxymethoxy; n R 3 is hydrogen, hydroxy, amino, methoxy, methoxymethyoxy, or taken together with R 2 , methylenedioxy (also known as 1,3-dioxolo); n R 4 is hydrogen, hydroxy, methoxy, methoxymethoxy, benzyl, di(C 1-4 )alkylaminomethyl or, taken together with R 3 , methylenedioxy; n R 5 is hydrogen or hydroxy; provided that at least one of R 1 through R 5 is other than hydrogen; and n i) X 2 is hydroxy or methoxy with X 1 , X 3 and X 4 being hydrogen; or n ii) X 1 taken together with X 2 , n X 2 taken together with X 3 or X 3 taken together with X 4 , is methylenedioxy, provided that each of the remaining respective X 1 , X 2 , X 3 and X 4 substituents are hydrogen, n intermediates in the synthesis of them, pharmaceutical formulation containing them, their use as inhibitors of topoisomerase and their use in the treatment of tumors.
摘要:Singh, F. V., Science of Synthesis Knowledge Updates, (2021) 1, 168. 摘要:Singh, F. V., Science of Synthesis Knowledge Updates, (2021) 1, 154. 摘要:Pilgrim, B. S.; Tucker, M. J., Science of Synthesis Knowledge Updates, (2019) 1, 237. 摘要:Collings, J. C., Science of Synthesis Knowledge Updates, (2013) 4, 306. 摘要:Sellars, J. D., Science of Synthesis Knowledge Updates, (2014) 1, 400.