CAS: 63610-09-3; 2-Amino-2-(Hydroxymethyl)Propane-1,3-Diol Hemi(2,2'-((2-Chloro-5-Cyano-1,3-Phenylene)Bis(Azanediyl))Bis(2-Oxoacetate))

📜诺朵腊酸,三羟甲基氨基甲烷 以 甲醇 作为反应溶剂,化学反应 0.5H,以73.6%的收率获得产物洛度沙胺氨丁三醇
参考文献:一种洛度沙胺氨丁三醇中间体的制备方法
标题:一种洛度沙胺氨丁三醇中间体的制备方法
摘要:本发明属于医药化工技术领域,具体公开了一种洛度沙胺氨丁三醇中间体洛度沙胺的制备方法,(1)将3,5‑二氨基‑4‑氯苯腈溶于有机溶剂中,形成溶液a;(2)将草酰氯溶于有机溶剂中,形成溶液b;(3)缓慢地将a溶液滴入b溶液中,滴加过程控制反应液温度在‑20oc~0°C,反应完毕后,将一定量的冰水缓慢滴加到反应液中,滴加完毕后继续搅拌0.5‑1H后抽滤,将所得滤饼烘干,即可得到洛度沙胺.本发明的反应步骤少,更有利于操作,收率得到了很大提升,收率可达到90%以上,同时产物洛度沙胺的相关杂质少,产品纯度高,HPLC纯度可达到99.5%以上,对洛度沙胺氨丁三醇药物的合成有重大意义.

专利信息

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:US-2012232031-A1
优先权日:2009-10-19
标 题:Injectable formulations for intra-articular or peri-articular administration
发明人：HUTCHINSON JOHN HOWARD; PRASIT PETPIBOON PEPPI; DEARMOND ISABELLE MARGUERITE
权利人:HUTCHINSON JOHN HOWARD; PRASIT PETPIBOON PEPPI; DEARMOND ISABELLE MARGUERITE; PANMIRA PHARMACEUTICALS LLC
摘要:Described herein are injectable formulations for intra-articular or peri-articular administration, wherein the formulation is administered to treat joint pain. An injectable formulation for intra-articular or peri-articular administration disclosed herein comprises a therapeutically-effective amount of a leukotriene synthesis inhibitor compound formulated for intra-articular or peri-articular administration.