CAS: 85622-93-1; 3-Methyl-4-Oxo-3,4-Dihydroimidazo[5,1-D][1,2,3,5]Tetrazine-8-Carboxamide

相似化合物

113942-30-6 85623-02-5 114601-31-9

上下游产品

methyl is°Cyanate 5-diazoimidazole-4-carboxamide (8-Carbamoyl-4-oxo-imidazo[5,1-d][1,2,3,5]tetrazin-3-yl)-acetic acid 2-thioxo-2H-pyridin-1-yl ester dimethyl sulfatemethanol2H1methan2Hol dimethylphosphoric acid deuteromethanol

以 N,N-二甲基甲酰胺 作为反应溶剂,以98.6%的收率获得产物替莫唑胺
参考文献:一种替莫唑胺的制备方法
标题:一种替莫唑胺的制备方法
摘要:本发明属于医药化工领域,具体涉及一种替莫唑胺的制备方法,本发明以亚硝基咪唑类化合物与甲基肼反应反应生成偶氮化合物iv,化合物iv进一步水解得中间体v,化合物v进一步与对硝基苯基氯甲酸酯亲核取代得到新中间体vii;中间体vii环合得替莫唑胺,该方法避免了毒性较大的异氰酸甲酯的使用和经历不稳定的重氮化合物中间体过程,且合成的中间体不会产生二聚杂质,以绿色催化剂代替传统催化剂,反应更加温和,经济环保且收率较高,适于工业化生产.

专利信息

专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-2015182634-A1
优先权日:2012-12-28
标 题:Molecular Design and Chemical Synthesis of Pharmaceutical-Ligands and Pharmaceutical-Pharmaceutical Analogs with Multiple Mechanisms of Action
发明人：COYNE CODY P; BEAR RYAN; JONES TONI
权利人:COYNE CODY P; BEAR RYAN; JONES TONI
摘要:Multi-phase and single-phase chemical reaction schemes have been developed for the synthesis of pharmaceutical-ligand analogs, pharmaceutical-pharmaceutical analogs, and similar molecular-molecular analogs that possess multiple mechanisms of action. The multi-phase organic chemical reaction schemes include relatively mild reaction conditions, high end product yields, and comparatively rapid completion of chemical reactions, which are all of particular utility for the synthesis of preparations including covalent pharmaceutical-receptor ligand or pharmaceutical-immunoglobulin analogs. Examples of pharmaceutical-ligand preparations that can be synthesized utilizing the multi-step chemical reaction schemes include covalent chemotherapeutic-ligand agents that possess selective targeted delivery properties and a capacity to exert additive and synergistic levels of cytotoxic anti-neoplastic potency. Pharmaceutical-pharmaceutical analogs, including chemotherapeutic-chemotherapeutic analogs that are capable of exerting multiple mechanisms of action, can be synthesized using either of the described multi-phase or single-phase organic chemistry reaction schemes. Each of these representative examples has utility against a spectrum of disease states including, for example, neoplastic conditions such as mammary adenocarcinoma/carcinoma, ovarian carcinoma, prostatic carcinoma, intestinal carcinoma, melanoma, leukemia, myeloma, and lymphoma.

专利号:US-2012177593-A1
优先权日:2009-07-20
标 题 :Synthesis of dendrimer conjugates
发明人：BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH
权利人:BAKER JR JAMES R; ZHANG YUEHUA; THOMAS THOMMEY P; DESAI ANKUR MAHESH; UNIV MICHIGAN
摘要:The present invention relates to novel methods of synthesis of therapeutic and diagnostic dendrimers. In particular, the present invention is directed to novel dendrimer conjugates, novel methods of synthesizing the same, compositions comprising the conjugates, as well as systems and methods utilizing the conjugates (e.g., in diagnostic and/or therapeutic settings (e.g., for the delivery of therapeutics, imaging, and/or targeting agents (e.g., in disease (e.g., cancer, inflammatory disease) diagnosis and/or therapy, pain therapy, etc.)). Accordingly, dendrimer conjugates of the present invention may further comprise at least two different components for targeting, imaging, sensing, and/or providing a therapeutic or diagnostic material and/or monitoring response to therapy. Furthermore, the novel synthesis methods of certain embodiments of the present invention provide significant advantages with regard to total reaction time and simplicity.

专利号:US-7173021-B2
优先权日:2004-09-02
标题:Synthesis of temozolomide esters as potent anticancer pro-drugs for topical and transdermal applications in treatments of cancers
发明人：WANG YONGFENG; CONWAY BARBARA R; SUPPASANSATORN PANASSAYA
权利人:TIANJIN NORTH PHARM SCI TECH C
摘要:This invention relates to the use of temozolomide esters (4-dihydro-3-methyl-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxylate esters) Formula 1 as potent anticancer pro-drugs for treatment of cancers by topical and transdermal applications, and to a novel process for synthesis of temozolomide esters by a direct esterification of temozolomide acid (3,4-dihydro-3-methyl-4-oxoimidazo[5,1-d]-1,2,3,5-tetrazine-8-carboxylic acid) with a halogeno-aliphatic compound in presence of a base, or with an alcohol in presence of a dehydrate agent

专利号:US-10973847-B2
优先权日:2017-06-30
标题 :Core-to-surface polymerization for the synthesis of star polymers and uses thereof
发明人：JOHNSON JEREMIAH A; GOLDER MATTHEW R
权利人:MASSACHUSETTS INST TECHNOLOGY
摘要:Disclosed are methods, compositions, reagents, systems, and kits to prepare star polymers, as well as compositions and uses thereof. Various embodiments show that synthesis of these polymers contain low metal concentration to provide polymers for diverse biomedical applications including in vivo applications.

专利号:WO-2018025074-A1
优先权日:2016-08-01
标题:Synthesis of new phosphorus dendrimers and use thereof
发明人：MAJORAL JEAN PIERRE; APARTSIN EVGENY; VENYAMINOVA ALYA; BRYSZEWSKA MARIA; IONOV MAKSIM; SHCHARBIN DZMITRY; DZMITRUK VOLHA; IHNATSYEU KACHAN ALIAKSEI
权利人:UNIV LODZKI
摘要:An object of this invention is synthesis of cationic phosphorus dendrimers of 3 rd and 4 th generation, possessing on the periphery the amino- and terminal functional P(S)C12 groups grafted with l-(2-aminoethyl)-piperidine and having the following structures where AE2G3H + stands for cationic phosphorus dendrimer of generation 3, AE2G4H + for cationic phosphorus dendrimer of generation 4. The invention covers also use of the dendrimers as delivery systems of the genetic material to cancer cells.