📜1-异丙基-5-苯基双胍置于氯体系中,化学反应生成 氯胍 参考文献:Crowther Et Al.,Journal Of The Chemical Society,1951,P. 1774,1778 标题:Crowther Et Al.,Journal Of The Chemical Society,1951,P. 1774,1778
专利号:US-8680276-B2 优先权日:2009-03-06 标题 :Synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine 发明人:MOTTERLE RICCARDO; ARVOTTI GIANCARLO; BERGANTINO ELISABETTA; CASTELLIN ANDREA; FOGAL STEFANO; GALVAGNI MARCO 权利人:MOTTERLE RICCARDO; ARVOTTI GIANCARLO; BERGANTINO ELISABETTA; CASTELLIN ANDREA; FOGAL STEFANO; GALVAGNI MARCO 摘要:The present invention relates to the stereoselective synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine, as well as the conversion thereof, to give Moxifloxacin. Particularly, the present invention relates to a method for the synthesis of (4aS,7aS)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) comprising: (a) the optical resolution by enzymatic hydrolysis of the intermediate dialkyl-1-alkylcarbonylpiperidine-2,3-dicarboxylate racemate of formula (II) to give, following isolation, the intermediate dialkyl-(2S,3R)-1-alkylcarbonyl-piperidine-2,3-dicarboxylate of formula (III) in which AIk is a straight or branched C1-C5 alkyl group; (b) the conversion of the intermediate (III) to (4aR,7aS)-1-alkylcarbonylhexahydrofuro[3,4-b]pyridine-5,7-dione of formula (IV) in which AIk has the meanings set forth above; (c) the conversion of the intermediate (IV) to (4aS,7as)-octahydro-1H-pyrrolo[3,4-b]pyridine of formula (I) with an optical purity above 99%.
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-7947701-B2 优先权日:2003-11-14 标题:Dual molecules containing peroxy derivative, the synthesis and therapeutic applications thereof 发明人:CAZELLES JEROME; COSLEDAN FREDERIC; MEUNIER BERNARD; PELLET ALAIN 权利人:SANOFI AVENTIS 摘要:The invention relates to dual molecule compounds containing a peroxide derivative, to processes for the synthesis of such compounds, to pharmaceutical compositions comprising such compounds, and to methods of treatment and prevention of malaria comprising administering such compounds and such pharmaceutical compositions.
专利号:US-4891430-A 优先权日:1984-12-04 标 题:Process for synthesizing active esters of carboxylic acids, new alpha-halogenated carbonates which are useful for this synthesis and the method of producing them 发明人:BARCELO GERARD; CASTRO BERTRAND; JAOUADI MAHMOUD; MARTINEZ JEAN; SENET JEAN-PIERRE; SENNYEY GERARD 权利人:INT DES POUDRES ET EXPLOSIFS S 摘要:The invention relates to a new process for preparing active esters or carboyxlic acids, which consists in reacting a carboxylic acid, in the presence of an agent for binding hydrohalic acid, with a carbonate of formula: ##STR1## in which R 1 denotes either a radical of formula ##STR2## in which R 3 and R 4 , which may be identical or different, are not hydrogen atoms and denote organic radicals which may be substituted or unsubstituted and saturated or unsaturated, and may or may not be bound to a polymer, and which can be joined together to form a hetero-cyclic system with the nitrogen, atom, n or a substituted or unsubstituted aryl radical which may or may not be bound to a polymer, n R 2 denotes a hydrogen atom, an aliphatic or cycloaliphatic radical which may be substituted or unsubstituted and saturated or unsaturated, or a substituted or unsubstituted aromatic radical, n and X denotes a halogen atom. n This process is especially useful for the synthesis of active esters of N-protected amino acids. The invention also relates to the new carbonates described above and the method of producing them, which consists in reacting an alpha-halogenated chloroformate of formula: n n R.sup.2 --CHX--O--COCl n n with an alcohol of formula R 1 OH in an inert solvent medium in the presence of an organic or inorganic base.
专利号:US-3708477-A 优先权日:1968-06-27 标 题:Process of total synthesis of cephalosporin derivatives and intermediates 发明人:MARTEL J; HEYMES R 权利人:ROUSSEL UCLAF 摘要:PROCESS FOR THE PREPARATION OF RACEMIC OR OPTICALLYACTIVE CEPHALOSPORINE DERIVATIVES OF THE FORMULA 2,3-(-CO-N(-R1)-CH2-),7-NH2-2-CEPHEM WHEREIN R1 IS A MEMBER SELECTED FROM THE GROUP CONSISTING OF HYDROGEN, ALKYL, SUBSTITUTED AKYL, ARYL AND SUBSTITUTED ARYL, WHICH COMPRISES THE STEPS OF REACTING AN AMINO ACID OF THE FORMULA R1-NH-CH2-CH2-COOH WITH BENZYL ALCOHOL, CONDENSING THE BENZYL ESTER THUS OBTAINED WITH AN OXALATE, CONVERTING THE BENZYL ESTER OF 2,3DIOXI-4-CARBOXY-PYRROLIDINE INTO THE CORRESPONDING ACID, SUBJECTING SAID ACID TO AMINOMETHYLATION, THUS YIELDING A COMPOUND OF THE FORMULA 1-R1,3-OH,4-(R'-N(-R'')-CH2-)PYRROL-3-IN-2-ONE CONVERTING SAID COMPOUND INTO THE CORRESPONDING 4-ACYLTHIOMETHYL DERIVATIVE, CONVERTING SAID DERIVATIVE INTO THE CORRESPONDING 4-THIOMETHYL DERIVATIVE, CONDENSING SAID DERIVATIVE WITH AN ENAMINE OF THE FORMULA R-OOC-C(-Y)=CH-NH2 TO OBTAIN A THIAZINE DERIVATIVE OF THE FORMULA 2-(Y-CH(-COO-R)-),5-R1-2,3,4,5,6,7-HEXAHYDRO-PYRROLO (3,4-D)-1,3-THIAZIN-4-ONE CONVERTING SAID THIAZINE DERIVATIVE INTO A COMPOUND OF THE FORMULA 2-(H2N-CH(-COOH)-),5-R1-2,3,4,5,6,7-HEXAHYDRO-PYRROLO (3,4-)-1,3-THIAZIN-4-ONE SUBJECTING SAID COMPOUND TO THE ACTION OF A TRITYLATION AGENT, RECOVERING THE THREO ISOMER OF THE TRITYLATED DERIVATIVE, LACTAMIZING SAID THREO ISOMER TO OBTAIN THE Y-LACTAM OF DL-6H,7H-CIS-7-TRITYLAMINO-3-AMINOALKYL-CEPH 3-EME-4-CARBOXYLIC ACID, DETRITYLATING SAID Y-LACTAM AND RECOVERING SAID RACEMIC OF OPTICALLY ACTIVE CEPHALOSPORIN DERIVATIVES. THESE COMPOUNDS ARE USEFUL AS INTERMEDIATES IN THE PREPARATION OF THE CORRESPONDING 7ACYLAMINO DERIVATIVES OF THE FORMULA 2,3-(-CO-N(-R1)-CH2-),7-(R2-NH-)-2-CEPHEM WHEREIN R1 HAS THE ABOVE DEFINITION AND R2 IS THE ACYL OF AN ORGANIC CARBOXYLIC ACID WHICH COMPOUNDS ARE ALSO PART OF THE INVENTION AND ARE USEFUL AS ANTIBIOTICS.
1: Ñacata I, Early AM, Boboy J, Neafsey DE, Sáenz FE. Effects of drug pressure and human migration on antimalarial resistance in circulating Plasmodium falciparum malaria parasites in Ecuador. Res Sq [Preprint]. 2024 Aug 16:rs.3.rs-4638168. doi: 10.21203/rs.3.rs-4638168/v1. 2: Drugs and Lactation Database (LactMed®) [Internet]. Bethesda (MD): National Institute of Child Health and Human Development; 2006–. Atovaquone and Proguanil. 2024 Jul 15. 10(8):2755-2774. doi: 10.1021/acsinfecdis.4c00113. Epub 2024 Jul 2. 39(22):e186. doi: 10.3346/jkms.2024.39.e186.
合成参考文献
参考文献:10.1155/2011/579518 摘要:Mishra K, Dash AP, Dey N. Andrographolide: A Novel Antimalarial Diterpene Lactone Compound fromAndrographis paniculataand Its Interaction with Curcumin and Artesunate. Journal of Tropical Medicine. 2011;2011():1–6. doi: 10.1155/2011/579518. 参考文献:10.1074/jbc.m111.269399 摘要:Boysen KE, Matuschewski K. Arrested Oocyst Maturation in Plasmodium Parasites Lacking Type II NADH:Ubiquinone Dehydrogenase. Journal of Biological Chemistry. 2011 Sep;286(37):32661–71. doi: 10.1074/jbc.m111.269399. 参考文献:10.1371/journal.pone.0021237 摘要:Penna-Coutinho J, Cortopassi WA, Oliveira AA, França TCC, Krettli AU. Antimalarial Activity of Potential Inhibitors of Plasmodium falciparum Lactate Dehydrogenase Enzyme Selected by Docking Studies. PLoS ONE. 2011 Jul 14;6(7):e21237. doi: 10.1371/journal.pone.0021237.