CAS: 171228-49-2; 4-(4-(4-(4-(((3R,5R)-5-((1H-1,2,4-Triazol-1-yl)Methyl)-5-(2,4-Difluorophenyl)Tetrahydrofuran-3-yl)Methoxy)Phenyl)Piperazin-1-yl)Phenyl)-1-((2S,3S)-2-Hydroxypentan-3-yl)-1H-1,2,4-Triazol-5(4H)-One

上下游产品

CAS号170985-86-1 O-苄基泊沙康唑 | CAS号106-41-2 对溴苯酚 | CAS号454479-36-8 (3S,3aS,7S,7aR)... | CAS号454479-39-1 2-((2S,3S)-2-(b... | CAS号171228-61-8 (2S,3R)-2-((ben... | CAS号51336-94-8 2-氯-2,4-二氟苯乙酮 | CAS号74853-08-0 1-(4-氨基苯基)-4-(4...

在 四丁基氟化铵,水体系中,用 四氢呋喃 用作溶剂,以80%的收率获得泊沙康唑
参考文献:泊沙康唑的制备方法
标题:泊沙康唑的制备方法
摘要:本发明公开如式所示可以作为抗真菌药泊沙康唑(Posaconazo Le)的制备方法.本发明的第一种制备方法是:采用化合物1为原料,经氨基保护得到化合物2,醇3在碱存在下与磺酰化试剂反应保护羟基得到化合物4,中间体2与三唑4在强碱条件下反应得到中间体5,然后在有机碱条件下与甲酰肼衍生物6缩合环化得到泊沙康唑关键中间体化合物7,经脱除保护基r2得到泊沙康唑;本发明的第二种制备方法是:将化合物2与化合物6在有机碱存在下发生环化反应得到化合物8,然后化合物8与化合物4在强碱作用下发生亲核取代反应得到化合物7,经脱除保护基r2得到泊沙康唑.

专利信息

专利号:US-12383499-B2
优先权日:2018-01-01
标题:Scale up synthesis of silicasome nanocarriers
发明人：NEL ANDRE E; MENG HUAN; LIU XIANGSHENG
权利人:UNIV CALIFORNIA
摘要:In order to facilitate the approval and commercialization of silicasome drug delivery systems (e.g. irinotecan silicasomes) it is necessary to scale up synthesis of the drug-loaded silicasomes. In this regard, it was discovered that the synthesis protocols used for laboratory synthesis of drug-loaded silicasomes (e.g., 500 mg/batch) do not scale to large scale silicasome production, because the resulting products were too heterogeneous for use as pharmaceuticals. Accordingly, new methods are provided herein that effectively afford the large-scale production of mesoporous silica nanoparticles (MSNPs) and lipid bilayer coated MSNPs (silicasomes).

专利号:US-10925977-B2
优先权日:2006-10-05
标 题 :Efficient synthesis of chelators for nuclear imaging and radiotherapy: compositions and applications
发明人：YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S
权利人:YANG DAVID J; YU DONGFANG; THOMPSON ANDREW S; CEIL POINT LLC; UNIV TEXAS
摘要:Novel methods of synthesis of chelator-targeting ligand conjugates, compositions comprising such conjugates, and therapeutic and diagnostic applications of such conjugates are disclosed. The compositions include chelator-targeting ligand conjugates optionally chelated to one or more metal ions. Methods of synthesizing these compositions in high purity are also presented. Also disclosed are methods of imaging, treating and diagnosing disease in a subject using these novel compositions, such as methods of imaging a tumor within a subject and methods of diagnosing myocardial ischemia.

专利号:US-2024336559-A1
优先权日:2021-10-06
标 题 :Anti-fungals compounds targeting the synthesis of fungal sphingolipids
发明人：OJIMA IWAO; HARANAHALLI KRUPANANDAN; DEL POETA MAURIZIO; GARG ASHNA
权利人:UNIV NEW YORK STATE RES FOUND
摘要:The present invention provides a compound having the structure: n n n n n n n n n n n n wherein n R 3 , R 4 , R 5 , R 6 , and R 7 are each independently, H, halogen, CN, —CF 3 , —OCF 3 , —NO 2 , alkyl, alkenyl, alkynyl, aryl, heteroaryl, heterocycle, —OH, —OAc, —OR 13 , —COR 13 , —CH 2 OR 13 , —SH, —SR 13 , —SO 2 R 13 , —NH 2 , —NHR 13 , —NR 14 R 15 , —NHCOR 12 , or —CONR 14 R 15 ; n R 9 , R 10 , R 11 , and R 12 are each independently, H, CN, alkenyl, alkynyl, aryl, heteroaryl, cycloalkyl, heterocycloalkyl, —OAc, —COR 13 , —SH, —SR 13 , —SO 2 R 13 , —NH 2 , —NHR 13 , —NR 14 R 15 , —NHCOR 12 , or —CONR 14 R 15 ;n wherein each occurrence of R 13 is independently alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein each occurrence of R 14 is independently —H, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, wherein each occurrence of R 15 is independently —H, alkyl, alkenyl, alkynyl, aryl, or heteroaryl, n n wherein when R 14 is methyl, R 15 is not methyl; n wherein at least one of R 9 , R 10 , R 11 , and R 12 is not H; n wherein at least one of R 3 , R 4 , R 5 , R 6 , and R 7 is not H.

专利号:US-9382288-B2
优先权日:2010-10-06
标题 :Derivatives of steroid benzylamines, having an antiparasitic antibacterial, antimycotic and/or antiviral action
发明人：BECKER KATJA; KRIEG REIMAR; SCHÖNECKER BRUNO
权利人:BECKER KATJA; KRIEG REIMAR; SCHÖNECKER BRUNO; UNIV GIESSEN JUSTUS LIEBIG
摘要:The present invention relates to compounds derived from steroids of the general formula (I) n nwherein L represents a linker and R # represents a steroid residue, the use of compounds of the general formula (I) in medicine and for the prophylaxis and/or the treatment of infectious diseases. Furthermore described are pharmaceutical compositions containing at least one compound of the general formula (I). A further aspect of the invention relates to the synthesis of said compounds of the general formula (I).

专利号:US-10443047-B2
优先权日:2014-05-01
标题 :Increasing cellular lipid production by increasing the activity of diacylglycerol acyltransferase and decreasing the activity of triacylglycerol lipase
发明人：TSAKRAKLIDES VASILIKI; BREVNOVA ELENA E
权利人:NOVOGY INC
摘要:Disclosed are methods and compositions for increasing the triacylglycerol content of a cell by up-regulating diacylglycerol acyltransferase and down-regulating triacylglycerol lipase. In some embodiments, a DGA1 protein is expressed and a native TGL3 gene is knocked out, thereby increasing the synthesis of triacylglycerol and decreasing its consumption, respectively.

专利号:US-12325678-B2
优先权日:2017-06-16
标 题 :Anti-fungals compounds targeting the synthesis of fungal sphingolipids
发明人：OJIMA IWAO; DEL POETA MAURIZIO; LAZZARINI CRISTINA; HARANAHALLI KRUPANANDAN; SUN YI
权利人:UNIV NEW YORK STATE RES FOUND
摘要:The present invention provides a compound having the structure: n nand use of the compound for inhibiting the growth of or killing.