CAS: 4085-31-8; 1,3-Bis(4-(7-Chloroquinolin-4-yl)Piperazin-1-yl)Propane

上下游产品

CAS号109-64-8 1,3-二溴丙烷 | CAS号837-52-5 7-氯-4-(1-哌嗪基)喹啉 | CAS号86-98-6 4,7-二氯喹啉

4,7-二氯喹啉置于三乙胺,Potassium Iodide体系中,用 甲醇,异丙醇 作为反应溶剂,化学反应 10.0H,反应生成 磷酸哌喹
参考文献: An Improved Process For The Preparation Of Piperaquine[fr] Procédé Amélioré Pour La Préparation De Pipéraquine
标题: An Improved Process For The Preparation Of Piperaquine[fr] Procédé Amélioré Pour La Préparation De Pipéraquine
摘要:本发明涉及一种改进的制备7-氯-4-哌嗪-1-基喹啉(化学式(i))的过程,该化合物是合成哌喋啶或其药用可接受盐的关键中间体.

专利信息

专利号:US-9206133-B2
优先权日:2011-06-06
标题:Process for the synthesis of 7-chloro-4-(piperazin-1-yl)-quinoline
发明人：CABRI WALTER; CASTAGNANI ROBERTO; ARMAROLI SILVIA; QUATTROCIOCCHI GIANANDREA; COLANGELI VINCENZO
权利人:CABRI WALTER; CASTAGNANI ROBERTO; ARMAROLI SILVIA; QUATTROCIOCCHI GIANANDREA; COLANGELI VINCENZO; SIGMA TAU IND FARMACEUTI
摘要:The present invention provides a new process of synthesis of a polymorph of 7-chloro-4-(piperazin-1-yl)-quinoline of Formula I. Said quinoline compound is substantially pure of any impurities. The present invention further provides the use of the above-mentioned polymorph of 7-chloro-4-(piperazin-1-yl)-quinoline in the synthesis of piperaquine or one of its pharmaceutically acceptable salts.

专利号:US-2012100555-A1
优先权日:2009-06-29
标题 :Synthesis And Use Of Fluorophore-Tagged Antimalarials
发明人：LEAR MARTIN JAMES; TAN KEVIN SHYONG WEI
权利人:LEAR MARTIN JAMES; TAN KEVIN SHYONG WEI
摘要:This invention includes a fluorophore-tagged antimalarial represented by the following structural formula (1) or a salt thereof. This invention relates to the synthesis of fluorophore-tagged antimalarials and describes the synthesis of a fluorophore-tagged antimalarial. These fluorophore-tagged antimalarials can be used to image live cells to determine the location of the antimalarial in the cell, identify drug resistance and growth related pathways in Plasmodium isolates, identify new drug targets and chemo-sensitizers to reverse drug resistance.

专利号:US-9409879-B2
优先权日:2011-03-29
标 题 :Total synthesis of redox-active 1.4-naphthoquinones and their metabolites and their therapeutic use as antimalarial and schistomicidal agents
发明人：DAVIOUD-CHARVET ELISABETH; LANFRANCHI DON ANTOINE; JOHANN LAURE; WILLIAMS DAVID LEE; CESAR RODO ELENA
权利人:DAVIOUD-CHARVET ELISABETH; LANFRANCHI DON ANTOINE; JOHANN LAURE; WILLIAMS DAVID LEE; CESAR RODO ELENA; CENTRE NAT RECH SCIENT
摘要:Naphthoquinones, azanaphthoquinones and benxanthones, their process of synthesis and methods of their use as antimalarial or antischistosomal agents.

专利号:US-9802952-B2
优先权日:2013-07-15
标 题:Method and apparatus for the synthesis of dihydroartemisinin and artemisinin derivatives
发明人：KOPETZKI DANIEL; MCQUADE DAVID TYLER; SEEBERGER PETER H; GILMORE KERRY
权利人:MAX-PLANCK-GESELLSCHAFT ZUR FÖRDERUNG DER WSS E V; MAX-PLANK-GESELLSCHAFT ZUR FÖRDERUNG DER WSS E V
摘要:The present invention is directed to a method for continuous production of dihydroartemisinin and also artemisinin derivatives derived from dihydroartemisinin by using artemisinin or dihydroartemisinic acid (DHAA) as starting material as well as to a continuous flow reactor for producing dihydroartemisinin as well as the artemisinin derivatives. It was found that the reduction of artemisinin to dihydroartemisinin in a continuous process requires a special kind of reactor and a special combination of reagents comprising a hydride reducing agent, at least one activator such as an inorganic activator, at least one solid base, at least one aprotic solvent and at least one C 1 -C 5 alcohol.

专利号:WO-2023187827-A1
优先权日:2022-03-30
标题:A pharmaceutical composition comprising an inhibitor of glutamine synthetase enzyme to combat artemisinin resistance in malaria
发明人：ARUN NAGARAJ VISWANATHAN; PADMANABAN GOVINDARAJAN; GHOSH SOURAV; KUNDU RAJIB; CHANDANA MANJUNATHA; ANAND ADITYA
权利人:INST OF LIFE SCIENCES
摘要:The present disclosure relates to a pharmaceutical composition to combat artemisinin resistance in malaria with the identification of Plasmodium falciparum (Pf) glutamine synthetase (GS) as a drug target. Pf Gs is important for maintaining asparagine levels in the parasite and promote protein synthesis. Since ART-resistant parasites undergo fitness loss in amino acid/nutrient- limiting conditions and GS levels are upregulated during ART exposure, targeting Pf GS and asparagine requirement can be harnessed to prevent ART resistance. The present disclosure also provides a method of suppressing the growth of Plasmodium falciparum and a method of treating malaria using GS inhibitors.

专利号:WO-2011095885-A1
优先权日:2010-02-08
标 题:An improved process for the preparation of piperaquine
发明人：SETHI MADHURESH KUMAR; RAWAT VIJENDRA SINGH; AYYARAN KARTHIKEYAN; YERRAMALLA RAJA KRISHNA; BONTALAKOTI JAGAN MOHAN RAO; VEMULA LAKSHMINARAYANA; NIMMAGADDA ANITHA; DATTA DEBASHISH
权利人:MATRIX LAB LTD; SETHI MADHURESH KUMAR; RAWAT VIJENDRA SINGH; AYYARAN KARTHIKEYAN; YERRAMALLA RAJA KRISHNA; BONTALAKOTI JAGAN MOHAN RAO; VEMULA LAKSHMINARAYANA; NIMMAGADDA ANITHA; DATTA DEBASHISH
摘要:The present invention relates to an improved process for the preparation of 7-chloro- 4-piperazin-1-yl-quinoline of formula (I), a key intermediate for the synthesis of Piperaquine or its pharmaceutically acceptable salts.