CAS: 137281-39-1; 4-(2-(2-Amino-4-Oxo-4,7-Dihydro-1H-Pyrrolo[2,3-D]Pyrimidin-5-yl)Ethyl)Benzoic Acid

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CAS号229470-22-8 4-[3-(2,4-diami... | CAS号65874-27-3 4-甲酰基苯甲酸叔丁酯 | CAS号146943-27-3 methyl 3-[4-(te... | CAS号151864-81-2 对乙氧基甲酰苯丙醛 | CAS号51934-41-9 对碘苯甲酸乙酯 | CAS号126931-32-6 tert-Butyl 4-(3... | CAS号134372-99-9 3-(4-[2,2-dimet... | CAS号146943-43-3 N-(4-(2-(2-氨基-4... | CAS号165049-28-5 N-(4-[2-(2-氨基-4...

4-(3-甲酰基丙基)苯甲酸乙酯置于盐酸,5,5-二溴-2,2-二甲基-4,6-二酮-1,3-二氧杂环己烷,Sodium Acetate,Sodium Hydroxide体系中,用 甲醇,乙醚,水 用作溶剂,化学反应 51.0H,反应生成培美酸
参考文献:Discovery Of 5-Substituted Pyrrolo[2,3-D]Pyrimidine Antifolates As Dual-Acting Inhibitors Of Glycinamide Ribonucleotide Formyltransferase And 5-Aminoimidazole-4-Carboxamide Ribonucleotide Formyltransferase In De Novo Purine Nucleotide Biosynthesis: Implications Of Inhibiting 5-Aminoimidazole-4-Carboxamide Ribonucleotide Formyltransferase To Ampk Activation And Antitumor Activity
标题:Discovery Of 5-Substituted Pyrrolo[2,3-D]Pyrimidine Antifolates As Dual-Acting Inhibitors Of Glycinamide Ribonucleotide Formyltransferase And 5-Aminoimidazole-4-Carboxamide Ribonucleotide Formyltransferase In De Novo Purine Nucleotide Biosynthesis: Implications Of Inhibiting 5-Aminoimidazole-4-Carboxamide Ribonucleotide Formyltransferase To Ampk Activation And Antitumor Activity
摘要:We Synthesized 5-Substituted Pyrrolo[2,3-D]Pyrimidine Antifolates (Compounds 5-10) With One-To-Six Bridge Carbons And A Benozyl Ring In The Side Chain As Antitumor Agents. Compound 8 With A 4-Carbon Bridge Was The Most Active Analogue And Potently Inhibited Proliferation Of Folate Receptor (Fr) Alpha-Expressing Chinese Hamster Ovary And Kb Human Tumor Cells. Growth Inhibition Was Reversed Completely Or In Part By Excess Folic Acid,Indicating That Fr Alpha Is Involved In Cellular Uptake,And Resulted In S-Phase Accumulation And Apoptosis. Antiproliferative Effects Of Compound 8 Toward Kb Cells Were Protected By Excess Adenosine But Not Thymidine,Establishing De Novo Purine Nucleotide Biosynthesis As The Targeted Pathway. However,5-Aminoimidazole-4-Carboxamide (Aica) Protection Was Incomplete,Suggesting Inhibition Of Both Aica Ribonucleotide Formyltransferase (Aicarftase) And Glycinamide Ribonucleotide Formyltransferase (Garftase). Inhibition Of Garftase And Aicarftase By Compound 8 Was Confirmed By Cellular Metabolic Assays And Resulted In Atp Pool Depletion. To Our Knowledge,This Is The First Example Of An Antifolate That Acts As A Dual Inhibitor Of Garftase And Aicarftase As Its Principal Mechanism Of Action.
Doi:10.1021/jm401328U

专利信息

专利号:US-8981090-B2
优先权日:2010-07-22
标 题:Process for the synthesis of pemetrexed disodium salt
发明人：CIAMBECCHINI UMBERTO; TURCHETTA STEFANO; ZENONI MAURIZIO; DE FERRA LORENZO; BRANDI PAOLO
权利人:CIAMBECCHINI UMBERTO; TURCHETTA STEFANO; ZENONI MAURIZIO; DE FERRA LORENZO; BRANDI PAOLO; CHEMI SPA
摘要:The present invention relates to a novel process for the preparation of pemetrexed diethyl ester 2 n nby purifying the mixture obtainable by reacting compounds 1 and 1a in the presence of a chemical agent capable of promoting the formation of a peptide bond in an aprotic organic solventn n ncharacterized in that the mixture is subjected to the following steps:n a) washing with a basic aqueous solution; b) concentration of the organic phase; c) addition of a polar organic solvent and/or a mixture of polar organic solvents; d) precipitation of the pemetrexed diethyl ester 2.

专利号:EP-2409978-A2
优先权日:2010-07-22
标 题 :A novel process for the synthesis of pemetrexed disodium salt

专利号:US-2012172595-A1
优先权日:2010-07-22
标题:Novel process for the synthesis of pemetrexed disodium salt

专利号:EP-2409978-B1
优先权日:2010-07-22
标 题 :A novel process for the synthesis of pemetrexed disodium salt

专利号:CN-1800183-A
优先权日:2004-12-30
标 题 :One-step synthesis process of key intermediate of pemetrexed disodium salt

专利号:CN-1800169-B
优先权日:2004-12-30
标 题:Key intermediate of pemetrexed disodium salt and synthesis method thereof, and method for synthesizing pemetrexed disodium salt from the intermediate