CAS: 154-93-8; 1,3-Bis(2-Chloroethyl)-1-Nitrosourea

该化合物是一种化学疗法中广泛使用的硝化苏尿碳合物剂,因为它能够跨越血脑屏障,能够有效地治疗脑肿瘤,包括血浆瘤多形和其他CNS恶性肿瘤,其机制包括对DNA和RNA进行烷基处理,抑制复制和转录,导致细胞迅速分解产生细胞毒性影响;卡穆斯因具有免疫压抑性,还用于在异形干细胞移植前的调节系统.该化合物存在于静脉和植入式长毛状配方中,在临床应用中具有灵活性.其亲身性能可以增强组织渗透性,但由于潜在的血解和肺毒性,需要仔细监测.

结构式图片

欧盟法规

ECHA物质C&L通报REACH预注册

上下游产品

CAS号2214-72-4 双氯乙基脲 | CAS号113900-20-2 1,2,2,2-Tetrach... | CAS号689-98-5 2-氯乙胺 | CAS号107-21-1 乙二醇 | CAS号75-07-0 乙醛 | CAS号107-07-3 2-氯乙醇 | CAS号2214-72-4 双氯乙基脲 | CAS号71353-16-7 N-(2-chloroethy... | CAS号2387-20-4 1-(2-氯乙基)-2-咪唑烷酮 | CAS号64-17-5 乙醇 | CAS号75-04-7 乙胺

合成工艺路线路线简述

    N,N'-双(2-氯乙基)脲置于四氯化锡,Sodium Nitrite体系中,用 二氯甲烷 用作溶剂,化学反应 2.0H,以100%的收率获得卡莫司汀
    参考文献:氯化锡(iv)-亚硝酸钠作为一种新的亚硝化剂,用于在温和和非均相条件下对胺,酰胺和脲进行 N-亚硝化
    标题:氯化锡(iv)-亚硝酸钠作为一种新的亚硝化剂,用于在温和和非均相条件下对胺,酰胺和脲进行 N-亚硝化
    摘要:我们开发了一种使用氯化锡 (Iv) 和硝酸钠的混合物对各种仲胺和叔胺,酰胺和脲进行 N-亚硝化的新方法.该方法通过原位生成亚硝酰氯 (Nocl) 实现选择性,高产和温和的非均相 N-亚硝化.该反应可以在几种不同的溶剂如氯仿,二氯甲烷,醚,乙酸乙酯和醇中,在室温下进行.
    Doi:10.1055/s-2006-942397

    海关参考信息

    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-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-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-5633260-A
    优先权日:1994-04-19
    标 题 :11,7 Substituted camptothecin derivatives and formulations of 11,7 substituted camptothecin derivatives and methods for uses thereof
    发明人:HAUSHEER FREDERICK H; HARIDAS KOCHAT
    权利人:BIONUMERIK PHARMACEUTICALS INC
    摘要:The novel compounds 11-hydroxy-7-ethyl camptothecin and 11-hydroxy-7-methoxy camptothecin (11,7-HECPT and 11,7-HMCPT) are active anticancer compounds which are poorly soluble in water. Because of their novelty, 11,7-HECPT and 11,7-HMCPT derivatives have not been directly administered by parenteral or oral routes to human subjects as an antitumor composition for the purpose of inhibiting the growth of cancer cells. The claimed compositions are useful as compared to the water soluble camptothecin derivatives, such as CPT-11, in clinical trials. The unpredictable interpatient variability in the metabolic production of an active metabolite from CPT-11 limits the utility of CPT-11. This invention overcomes these limitations by claiming novel pharmaceutically acceptable lactone stable formulations of 11,7-HECPT or 11,7-HMCPT, to directly administer to patients. The present invention also claims 11,7-HECPT and 11,7-HMCPT compositions, the synthesis of 11,7-HECPT or 11,7-HMCPT, the methods of formulation of 11,7-HECPT or 11,7 -HMCPT, and the methods of use of 11,7-HECPT or 11,7-HMCPT. Additionally, the claimed invention is directed to novel dosages, schedules, and routes of administration for both the 11,7-HECPT or 11,7-HMCPT formulations to humans with various forms of cancer. Other embodiments of this invention include isolation methods and methods of synthesis of certain camptothecin derivatives.

    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-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.
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    主要参考文献


    1: Rahimi SM, Bagheri A. Critical regulatory roles of non-coding RNAs in driving cancer sensitivity to Carmustine: a systematic review. Naunyn Schmiedebergs Arch Pharmacol. 2026 Feb;399(3):3335-3352. doi: 10.1007/s00210-025-04562-5. Epub 2025 Oct 23.
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    合成参考文献


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    参考文献:10.1038/ncomms1382|10.2210/pdb3qfa/pdb|10.2210/pdb3qfb/pdb
    摘要:Fritz-Wolf K, Kehr S, Stumpf M, Rahlfs S, Becker K. Crystal structure of the human thioredoxin reductase-thioredoxin complex. Nat Commun. 2011 Jul 12;2():383. doi: 10.1038/ncomms1382.
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