CAS: 2211-57-6; N-Benzylguanidine

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CAS号108123-81-5 Ethyl 2-(benzyl... | CAS号104296-01-7 6-Amino-2-(benz... | CAS号89242-69-3 N-benzyl-4-meth...

📜在 Sodium Hydride体系中,用 1,4-二氧六环,N,N-二甲基甲酰胺 用作溶剂,化学反应 0.33H,反应生成苄基胍半硫酸盐
参考文献:Ligustrazine Derivatives. Part 6: Design,Synthesis And Evaluation Of Novel Ligustrazinyl Acylguanidine Derivatives As Potential Cardiovascular Agents
标题:Ligustrazine Derivatives. Part 6: Design,Synthesis And Evaluation Of Novel Ligustrazinyl Acylguanidine Derivatives As Potential Cardiovascular Agents
摘要:A Series Of Novel Ligustrazinyl Acylguanidines Was Designed,Synthesized And Evaluated For Their Protective Effect On Injured Vascular Endothelial Cell (Ecv-304). The Preliminary Results Demonstrated That Some Compounds Possessed More Potent Activities Than That Of Ligustrazine In Stimulating Replication Of The Injured Endothelial Cell. Among The Active Compounds,Compounds 8B,8F And 8L Displayed Remarkable Antioxidative Activity With Low Ec50 Values Of 0.097,0.059 And 0.094 Mm,Respectively. Structure-Activity Relationships Were Briefly Discussed.
Doi:10.2174/157340612802084243

专利信息

专利号:US-4388310-A
优先权日:1982-03-01
标 题:6-Amido-2-S-oxides of substituted 2-organothio-pen-2-em-3-carboxylic acids
发明人：CHRISTENSEN BURTON G; DININNO FRANK P; MUTHARD DAVID A; RATCLIFFE RONALD W
权利人:MERCK & CO INC
摘要:Disclosed are 6-amido-2-S-oxides of substituted 2-organothio-pen-2-em-3-carboxylic acids (I) which are useful as antibiotics and as intermediates in the synthesis of substituted pen-2-em-3-carboxylic acids: I wherein: R1 is H or acyl; R2 is hydrogen or methoxyl; R3 is alkyl having from 1-6 carbon atoms; phenylalkyl having 7-12 carbon atoms; and cycloalkyl having 3-6 carbon atoms; and R4 is hydrogen, a removable protecting group or a pharmaceutically acceptable salt or ester moiety.

专利号:US-8076499-B2
优先权日:2009-08-13
标 题 :Method for preparing precursor of radioactive 3-iodobenzylguanidine
发明人：LIU SHOW-WEN; LIN CHENG-HSIEN; LIN TSYH-LANG; HSU CHENG-FANG
权利人:LIU SHOW-WEN; LIN CHENG-HSIEN; LIN TSYH-LANG; HSU CHENG-FANG; ATOMIC ENERGY COUNCIL
摘要:A method for preparing a precursor of radioactive 3-iodobenzylguanidine- N,N′-bis(tert-butyloxycarbonyl)-3-(tri-n-butyltin)benzylguanidine) (MSnBG) is revealed. The method includes following steps. Firstly, obtain 3-iodobenzylguanidine bicarbonate by an addition reaction between 3-iodobenzylamine hydrochloride and cyanamide. Use di-tert-butyl dicarbonate as a protecting agent for NH group and convert 3-iodobenzylguanidine bicarbonate into N,N′-bis(tert-butyloxycarbonyl)-N-(3-iodobenzyl) guanidine. At last, under catalysis of bis(triphenylphosphine) palladium dichloride, obtain a final product MSnBG by a substitution reaction between N,N′-bis(tert-butyloxycarbonyl)-N-(3-iodobenzyl) guanidine and bis(tri-n-butyltin). MSnBG is used in no-carrier-added synthesis of [*l]MIBG.

专利号:US-11186551-B2
优先权日:2020-04-29
标题 :Composition of scalable thyrointegrin antagonists with improved retention in tumors
发明人：MOUSA SHAKER A; HAY BRUCE A
权利人:NANOPHARMACEUTICALS LLC
摘要:Chemical compounds/compositions, methods of synthesis, and methods of use. The compounds/compositions are directed toward thyrointegrin antagonists conjugated to a polymer. The compounds/compositions further comprise an additional substituent also conjugated to the polymer. The compounds/compositions demonstrate increased uptake across the blood brain barrier along with increased retention therein and retention within tumor. The compounds/compositions may also include improved synthesis scalability, improved purity, improved aqueous solubility, and a solid product or intermediate. The compounds/compositions may demonstrate improved antiangiogenic effect and improved efficacy against conditions, particularly cancers, requiring blood brain barrier permeability, for example, glioblastoma (GBM).

专利号:US-9550000-B2
优先权日:2011-09-09
标题 :Compositions, methods, and systems for the synthesis and use of imaging agents
发明人：ROBINSON SIMON P; YU MING
权利人:ROBINSON SIMON P; YU MING; LANTHEUS MEDICAL IMAGING INC
摘要:The present invention relates to systems, compositions, and methods for the synthesis and use of imaging agents, or precursors thereof. An imaging agent precursor may be converted to an imaging agent using the methods described herein. In some cases, the imaging agent is enriched in 18 F. In some cases, an imaging agent may be used to image an area of interest in a subject, including, but not limited to, the heart, cardiovascular system, cardiac vessels, brain, and other organs. In some embodiments, methods and compositions for assessing perfusion and innervation mismatch in a portion of a subject are provided.

专利号:WO-2022260918-A1
优先权日:2021-06-07
标 题:Composition and method for dual targeting in treatment of neuroendocrine tumors
发明人：MOUSA SHAKER; RAJABI MEHDI; KARAKUS OZLEM O
权利人:NANOPHARMACEUTICALS LLC
摘要:Chemical compositions and methods of synthesis thereof. The compositions disclosed and described herein are directed toward thyroid hormone ανβ3 integrin receptor antagonists conjugated to targets of the norepinephrine transporter (NET) or the catecholamine transporter. The compositions have a dual targeting effect and increased targeting efficiency in the treatment and diagnostic imaging of neuroendocrine tumors.

专利号:US-10053423-B2
优先权日:2014-01-03
标 题:Radioiodinated compounds
发明人：DIMAGNO STEPHEN; HU BAO
权利人:NUTECH VENTURES
摘要:This disclosure relates to reagents and methods useful in the synthesis of aryl iodines, for example, in the preparation of iodine labeled radiotracers. The reagents and methods provided herein may be used to access a broad range of compounds, including aromatic compounds, heteroaromatic compounds, amino acids, nucleotides, and synthetic compounds.