CAS: 55-86-7; Chlormethine (Hydrochloride)

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2,2'-(甲基亚胺)二乙醇盐酸盐置于氯化亚砜体系中,用 氯仿 作为反应溶剂,化学反应 2.0H,以99%的收率获得产物恩比兴
参考文献:'3+1' Mixed-Ligand Oxotechnetium(V) Complexes With Affinity For Melanoma: Synthesis And Evaluation In Vitro And In Vivo
标题:'3+1' Mixed-Ligand Oxotechnetium(V) Complexes With Affinity For Melanoma: Synthesis And Evaluation In Vitro And In Vivo
摘要:**'3+1'型杂配位体[tc-99M]氧肟technetium复合物的合成及其对黑色素瘤的靶向性研究** 在一步锅法反应中,成功合成了一种对黑色素瘤具有亲和力的'3+1'型杂配位体 [tc-99M]Oxotechnetium 复合物.通过将 Technetium-99M 与 N-R(3-氮杂戊烷-1,5-二硫醇)[r = Me,Pr,Bn,Et2N(Ch2)2] 和 N-(2-双烷基氨基)乙烷硫醇 [烷基 = X = Et,Bu,吗啉基] 的混合物中的 Technetium-99M 复合,并使用 Sn²+ 作为还原剂,最终形成了'3+1'型杂配位体 Technetium-99M 复合物 [tco(Sn(R)S)(Snx2)],其放射化学产率高达 60-98% . 体外实验中,利用 B16 小鼠黑色素瘤细胞进行的摄取研究表明,化合物 1 [r = Me,X = Et] 在60 分钟孵育后的肿瘤细胞积聚量为 40%,而化合物 2 [r = Me,X = Bu] 则达到了 69% 的较高积聚量.在 C57B16/b16 小鼠黑色素瘤模型中,对化合物 1-6 进行的体内评估显示,这些化合物均表现出肿瘤定位能力.其中,化合物 2 在注射后60 分钟内达到最高的积聚量,为 5% Id/g . 进一步的体内研究表明,化合物 2 在1 小时时表现出较低的血液活性,并且其黑色素瘤/脾脏(4.3)和黑色素瘤/肺(1.9)比值显著升高.这些结果表明,小巧的 Technetium-99M 复合物有望成为潜在的黑色素瘤成像剂.
DOI:10.1021/jm000050E

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-4334969-A
优先权日:1980-07-04
标题 :Photochemical process for the synthesis of strobilurin
发明人：STEGLICH WOLFGANG; SCHRAMM GEORG; ANKE TIMM; OBERWINKLER FRANZ
权利人:HOECHST AG
摘要:Process for stereoselective synthesis of strobilurin in the (E) configuration, starting from cinnamaldehyde and 2-oxobutyric acid.

专利号:WO-2017051326-A1
优先权日:2015-09-23
标 题 :New processes and intermediates useful in synthesis of nep inhibitors
发明人：MARTIN BENJAMIN; PENN GERHARD; SCHENKEL BERTHOLD; BOURNE SAMUEL; LAU SHING-HING; LEY Steven
权利人:NOVARTIS AG; MARTIN BENJAMIN; PENN GERHARD; SCHENKEL BERTHOLD; BOURNE SAMUEL; LAU SHING-HING; LEY Steven
摘要:The invention relates to a novel process, novel process steps and novel intermediates useful in the synthesis of pharmaceutically active compounds, in particular neutral endopeptidase (NEP) inhibitors such as sacubitril, and prodrugs thereof.

专利号:US-8734846-B2
优先权日:2008-06-16
标 题 :Methods for the preparation of targeting agent functionalized diblock copolymers for use in fabrication of therapeutic targeted nanoparticles
发明人：ALI MIR M; HRKACH JEFF; ZALE STEPHEN E; ALVAREZ DE CIENFUEGOS LUIS
权利人:BIND BIOSCIENCES INC
摘要:This application provides nanoparticles and methods of making nanoparticles using pre-functionalized poly(ethylene glycol)(also referred to as PEG) as a macroinitiator for the synthesis of diblock copolymers. Ring opening polymerization yields the desired poly(ester)-poly (ethylene glycol)-targeting agent polymer that is used to impart targeting capability to therapeutic nanoparticles. This “polymerization fromâ€? approach typically employs precursors of the targeting agent wherein the reactivity of functional groups of the targeting agent is masked using protecting groups. Also described is a “coupling toâ€? that utilized the poly(ethylene glycol)-targeting agent conjugate where the targeting agent remains in its native un-protected form. This method uses “orthogonalâ€? chemistry that exhibit no cross reactivity towards functional groups typically found within targeting agents of interest.

专利号:EP-1532112-B1
优先权日:2002-07-19
标 题 :Process for the preparation of modification i of n-(1-methylethylaminocarbonyl)-4-(3-methylphenylamino)-3-pyridinesulfonamide
发明人：FILIC DARKO; DUMIC MILJENKO; DANILOVSKI ALEKSANDAR; KLEPIC BOZENA; FISTRIC INES; MARINKOVIC MARINA; HORVAT-MIKULCIC JASNA
权利人:PLIVA HRVATSKA D O O
摘要:The invention relates to a new process for the preparation of modification I of torasemide by precipitation with acids from an alkaline extract of the original reaction mixture of the last phase in the synthesis of torasemide.

专利号:US-2013035307-A1
优先权日:2010-01-26
标 题:Methods for treating or preventing the spread of cancer using semi-synthetic glycosaminoglycosan ethers
发明人：PRESTWICH GLENN D; KENNEDY THOMAS P
权利人:UNIV UTAH RES FOUND; PRESTWICH GLENN D; KENNEDY THOMAS P
摘要:Described herein are methods for the treatment and prevention of tumor metastasis using alkylated and fluoroalkylated semi-synthetic glycosaminoglycan ethers (“SAGEsâ€?). The synthesis of sulfated alkylated and fluoroalkylated SAGEs is also described.