CAS: 937-13-3; 4,6-Dioxo-1,4,5,6-Tetrahydro-1,3,5-Triazine-2-Carboxylic Acid

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CAS号99-16-1 尿囊酸 | CAS号108-80-5 氰尿酸

尿囊酸置于氢氧化钾,Potassium Permanganate体系中,用 水 作为反应溶剂,化学反应 2.0H,反应生成 2,4-二羟基-1,3,5-三嗪-6-羧酸
参考文献:尿酸转化为尿烷酸酯和尿囊素的机制:一种新的碱诱导的1,2-羧酸盐转移
标题:尿酸转化为尿烷酸酯和尿囊素的机制:一种新的碱诱导的1,2-羧酸盐转移
摘要:通过同位素位置标记研究了尿酸的碱性高锰酸盐氧化(1),特别是转化为尿烷酸酯(7)和尿囊素(3)的后期.开发出的用于区分这些产品中的羰基和α-氨基碳原子的清晰降解程序明确证明了7的羧基碳和3的4-羰基碳起源于尿酸的c(5)(1) .对于该反应提出的机制均未预料到该结果.同位素标记的证据与其他数据结合,揭示了1的氧化转化所涉及的物种的事件和身份的序列.第一过渡中间体4的碳骨架重排必须发生1,
DOI:10.1016/s0040-4020(01)90112-7

专利信息

专利号:US-12391691-B2
优先权日:2018-11-16
标题:Synthesis of key intermediate of KRAS G12C inhibitor compound
发明人：PARSONS ANDREW THOMAS; COCHRAN BRIAN MCNEIL; POWAZINIK IV WILLIAM; CAPORINI MARC ANTHONY
权利人:AMGEN INC
摘要:The present invention relates to an improved, efficient, scalable process to prepare intermediate compounds, such as compound 5M, having the structure n nuseful for the synthesis of compounds that target KRAS G12C mutations, such as

专利号:US-2025206736-A1
优先权日:2019-11-14
标题 :Synthesis of kras g12c inhibitor compound
发明人：CORBETT MICHAEL THOMAS; CAILLE SEBASTIEN
权利人:AMGEN INC
摘要:The present disclosure relates to an improved, efficient, scalable process to prepare intermediate compounds, such as 2-isopropyl-4-methylpyridin-3-amine, useful for the synthesis of compounds, such as Compound 9, for the treatment of KRAS G12C mutated cancers.

专利号:US-2005080260-A1
优先权日:2003-04-22
标 题 :Preparation of prodrugs for selective drug delivery
发明人：MILLS RANDELL L; WU GUO-ZHANG
摘要:Synthesis of a chemical compound having the formula A-B-C that may serve for applications such as drug delivery where A is a chemiluminescent, moiety, B is a photochromic moiety, and C is a biologically active moiety where A-B-C may serve as a prodrug. Novel synthetic methods of the present invention to form the prodrug comprised the steps of (1) forming a benzophenone, (2) forming a diaryl ethylene, (3) attaching a phthalimide moiety to at least one of the aryl groups of the ethylene to form a phthalimide-ethylene conjugate, (4) condensing two ethylene-phthalimide conjugates to form a phthalimide-pentadiene conjugate, (5) converting the phthalimide to the phthalhydrazide by reaction with hydrazine to form a carrier compound according to the present invention, and (6) reacting the carrier compound with an nucleophilic moiety of the drug to form the corresponding prodrug. Alternatively the carrier can be prepared by using the halo-substituted diaryl ethylene to make the corresponding cationic leuco dye-like compound with known methods. The cationic compound then is protected by reacting with a nucleophile and coupled with the aminophathalimide by palladium-catalyzed amination to form the protected phthalimide-pentadiene conjugate. The latter is refluxed with hydrazine to convert its phthalimide to the phthalhydrazide and acidified to give the carrier. An additional aspect of the present invention relates to the use of these compounds as antiviral agents for the treatment of viral infections such as HIV and as anticancer agents for the treatment of cancers such as bowel, lung, and breast cancer.

专利号:US-8513417-B2
优先权日:2007-01-31
标题 :Method for synthesis of nitroxyl radical
发明人：UTSUMI HIDEO; SAKAI KIYOSHI; YAMADA KENICHI
权利人:UTSUMI HIDEO; SAKAI KIYOSHI; YAMADA KENICHI; UNIV KYUSHU NAT UNIV CORP
摘要:The problem to be solved by the present invention is to provide a highly-versatile method for producing a nitroxyl radical derivative, in which position-2 and position-6 in a TEMPO-based compound can be easily substituted, and further, a method for producing a nitroxyl radical derivative, in which a nitrogen nucleus is labeled with 15 N. The above-described problem can be solved by reacting a triacetoneamine derivative with ketone or aldehyde in the presence of ammonium salt or a 15 N-labeled compound thereof to obtain a 2,6-substituted-4-piperidone derivative.

专利号:US-4469895-A
优先权日:1982-10-21
标题 :Process for preparing alcohols from olefins and synthesis gas
发明人：KNIFTON JOHN F; GRIGSBY JR ROBERT A
权利人:TEXACO INC
摘要:This invention concerns an improved process of preparing predominantly linear alcohols which comprises the steps of contacting a mixture of terminal and/or internal olefins and synthesis gas with a catalyst system comprising a ruthenium-containing compound in conjunction with one or more tertiary amine promoters, dispersed in a low melting quaternary phosphonium salt and heating said resultant reaction mixture under a pressure of 100 psi or greater at a temperature of at least 50 DEG C. for a sufficient time to produce said alcohols.

专利号:US-2022118123-A1
优先权日:2019-02-22
标 题 :Combination of ar antagonists and targeted thorium conjugates
发明人：HAMMER STEFANIE; HAGEMANN URS BEAT; HAENDLER BERNARD; LEJEUNE PASCALE; ZITZMANN-KOLBE SABINE; SCHATZ CHRISTOPH; KARLSSON JENNY
权利人:BAYER AG; BAYER AS
摘要:The present invention covers combinations of at least two components, component A and component B, comprising component A being PSMA-TTC, and component B being an antiandrogen selected form AR antagonists such as from cyproterone acetate, bicalutamide, flutamide, nilutamide, enzalutamide, apalutamide, darolutamide or keto-darolutamide, or an AR degrader such as ARV-110, or an ARN-terminal domain binder such as EPI-506, or an antisense oligonucleotide that reduces AR expression such as EZN-4176 or AZD-5312, or an androgen synthesis inhibitor such as abiraterone, particularly abiraterone acetate, seviteronel, galeterone, orteronel or ketoconazole, or a dual AR antagonist and androgen synthesis inhibitor such as ODM-204. Another aspect of the present invention covers the use of such combinations as described herein for the preparation of a medicament for the treatment or prophylaxis of a disease, particularly for the treatment of a hyper-proliferative disease.