CAS: 13010-47-4; 1-(2-Chloroethyl)-3-Cyclohexyl-1-Nitrosourea

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CAS号13908-11-7 1-环己基-3-(2-氯乙基)脲 | CAS号76310-06-0 N-cyclohexyl-3-... | CAS号80354-49-0 CARBAMIC ACID, ... | CAS号108-91-8 环己胺 | CAS号80354-51-4 (2,4,5-trichlor... | CAS号80354-53-6 (2,3,4,5,6-pent... | CAS号80354-55-8 pentafluorophen... | CAS号55661-43-3 4-nitrophenyl-N... | CAS号10002-37-6 2-Oxazolamine,N... | CAS号3173-53-3 环己基异氰酸酯 | CAS号107-21-1 乙二醇 | CAS号75-07-0 乙醛 | CAS号107-07-3 2-氯乙醇

N-环己基-3-亚硝基-1,3-恶唑烷-2-亚胺置于盐酸体系中,用 乙醚 用作溶剂,化学反应 0.5H,以43%的收率获得洛莫司汀
参考文献:(2-卤代乙基)亚硝基脲对dna的作用机理.1,3-双(2-氯乙基)-,1-(2-氯乙基)-3-环己基-和1-(2-)分解中假定的2-(烷基亚氨基)-3-亚硝基恶唑烷中间体的分离和反应氯乙基)-3-(4'-反式甲基环己基)-1-亚硝基脲.
标题:(2-卤代乙基)亚硝基脲对dna的作用机理.1,3-双(2-氯乙基)-,1-(2-氯乙基)-3-环己基-和1-(2-)分解中假定的2-(烷基亚氨基)-3-亚硝基恶唑烷中间体的分离和反应氯乙基)-3-(4'-反式甲基环己基)-1-亚硝基脲.
摘要:制备了三个假定的但迄今尚未分离的2-(烷基亚氨基)-3-亚硝基恶唑烷(2)的实例,它们分别在2位含有环己基,反式-4-甲基环己基和2-氯乙基.这些化合物对应于先前假定在抗肿瘤剂1-(2-氯乙基)-3-环己基-(ccnu),1-(2-氯乙基)-3-(4'-反式-甲基环己基)-(meccnu)和1,3-双(2-氯乙基)-1-亚硝基脲(bcnu),化合物2在生理条件下分解,得到的一系列产物与相应的(2-氯乙基)亚硝基脲,包括迄今无法识别的2-羟基乙基n-烷基氨基甲酸酯(9).用盐酸将化合物2A和2B分别转化为ccnu和meccnu,提示2A和2B可能是分解的反应中间体.表征了相应的3-烷基-1-亚硝基-1-(2-羟乙基)脲(4),由于它们也分解产生与2相同的产物,因此可能是由于2的开环而引起的.图4可以解释由其他工作者从(2-氯乙基)亚硝基脲在多核苷酸上的反应分离的羟乙基化核苷的形成.
Doi:10.1021/jm00135A007

专利信息

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-7816544-B2
优先权日:2004-03-23
标 题:Synthesis of rocaglamide natural products via photochemical generation of oxidopyrylium species
发明人：JONES II GUILFORD; GERARD BAUDOUIN; PORCO JR JOHN A
权利人:UNIV BOSTON
摘要:The present invention provides new strategies for the synthesis of compounds of the rocaglamide family and related natural products. In particular, the new biomimetic synthetic approach involves photochemical generation of an oxidopyrylium species from a 3-hydroxychromone derivative followed by 1,3-dipolar cycloaddition of the oxidopyrylium species to a dipolarophile. This approach can be used for the formation of adducts containing an aglain core structure. Methods for the conversion of aglain core structures to aglain, rocaglamide and forbaglin ring systems are also provided. The present invention also relates to the use of rocaglamide/aglain/forbaglin derivatives for the manufacture of medicaments for use in the treatment of cancer or cancerous conditions, disorders associated with cellular hyperproliferation, or NF-κB-dependent conditions.

专利号:US-10975069-B2
优先权日:2014-04-01
标 题 :Sigma-2 receptor ligand drug conjugates as antitumor compounds, methods of synthesis and uses thereof
发明人：HAWKINS WILLIAM; MACH ROBERT; SPITZER DIRK; VANGVERAVONG SUWANNA; VAN TINE BRIAN
权利人:UNIV WASHINGTON
摘要:Methods and compositions for treating cancers such as pancreatic cancer and synovial sarcoma are disclosed. Compounds comprising a sigma-2 receptor-binding moiety and a ferroptosis-inducing moiety are described, such as the methanesulfonate salt of a compound of structural Formula IV, n n, wherein n is an integer chosen from 1, 2, 3, 4, and 5, and R 2 is H or methyl. At least one described molecular species exhibits an IC 50 value below 5 μM against human pancreatic cancer cells in vitro. Administration of this species promoted shrinkage of pancreatic cancer tumors in a murine model system in vivo. It led to a 100% survival of experimental animals over a time course in which control therapies provided only 30% or 40% survival. Methods of synthesis of molecular species are also disclosed.

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-2023192601-A1
优先权日:2020-05-11
标 题:Scaled-up synthesis of lomustine under control flow conditions
发明人：THOMPSON DAVID HARLEY; Nagy Zoltan Kalman; MUFTI AHMED; MACKEY JARON
权利人:PURDUE RESEARCH FOUNDATION
摘要:The present disclosure provides processes and apparatuses for the scaled-up manufacture of lomustine via continuous flow manufacture. Such continuous flow processes may optionally include the crystallization of lomustine and the apparatuses may optionally include crystallization apparatuses/reactors in either batch or continuous flow design. In one aspect of the disclosure, a process for making lomustine is provided comprising treating solutions of 2-chloroethylisocyanate with a solution of cyclohexylamine with continuous-flow pumps in a gram-flow reactor to form a combined solution, adding deionized water with a continuous flow-pump to the combined solution to form a liquid-organic phase solution, extracting the organic phase from the solution and treating with a solution of t-butyl nitrite with a continuous flow pump in a gram flow reactor to form lomustine.

专利号:US-2025009786-A1
优先权日:2021-09-30
标 题 :Automated synthesis of polymeric dual drugs
发明人：MATRAY TRACY; VANBRUNT MICHAEL; MCCUTCHEON JOHN MICHAEL
权利人:SONY GROUP CORP
摘要:Compounds useful as biologically active compounds with or without fluorescent or colored dyes are disclosed. In some embodiments, the compounds have the following structure (I): (I) or a stereoisomer, tautomer or salt thereof, wherein R1, R2, R3, R4, R5, R6, R7, L1, L2, L3, L4, L5, L6, L7, L8, L9, L10, L11, M1, M2, M3, l, m, n, p, and q are as defined herein. Additional compound, methods of preparation, pharmaceutical compositions, and methods of treatment related to compounds of Structure (I) are also provided.