CAS: 61318-90-9; 1-(2-((4-Chlorobenzyl)Thio)-2-(2,4-Dichlorophenyl)Ethyl)-1H-Imidazole

Alpha-(2,4-二氯苯基)-1H-咪唑-1-乙醇置于氯化亚砜,五羰基铁体系中,化学反应 19.0H,反应生成 硫康唑
参考文献:铁催化卤化苄和二硫化物的交叉电偶合
标题:铁催化卤化苄和二硫化物的交叉电偶合
摘要:交叉亲电子偶联是有影响的反应,通常需要末端还原剂或光氧化还原条件.我们发现了一种铁催化反应,在没有末端还原剂的情况下,在光氧化还原条件下,苄基卤与二硫化物偶联反应生成硫醚产物.所公开的平台无需硫引起的催化剂中毒或使用外源碱,支持广泛的范围并避免不期望的消除途径.我们将开发的化学方法应用于二硫键生物共轭,药物合成,克级合成和产品衍生化的新模式.最后,我们进行了机械实验,以更好地了解两种亲电子试剂之间的立体消融反应.二硫化物和苄基硫醚对于生物和制药应用至关重要,但与醚类和氨基对应物相比,其研究仍然严重不足.因此,我们预计这个铁催化平台和下游应用会引起更大的科学界的兴趣.
DOI:10.1021/jacs.3C13984

专利信息

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-8557979-B2
优先权日:2004-06-10
标题 :Carbapenem antibacterials with gram-negative activity and processes for their preparation
发明人：CHOI WOO-BAEG; KOWALIK EWA
权利人:CHOI WOO-BAEG; KOWALIK EWA; FOB SYNTHESIS INC
摘要:The present invention provides β-methyl carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment. The present invention is also in the field of synthetic organic chemistry and is specifically provides an improved method of synthesis of β-methyl carbapenems which are useful as antibacterial agents.

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-10933051-B2
优先权日:2017-06-09
标 题 :Carbapenem compounds and compositions for the treatment of bacterial infections
发明人：CHOI WOO-BAEG; TOMIOKA TAKASHI; JOO HYUNG-YEUL; TRUONG PHONG; MIN BRIAN
权利人:FOB SYNTHESIS INC
摘要:The present invention provides carbapenem compounds and pharmaceutical compositions useful in the treatment of bacterial infections, including drug resistant or multiple-drug resistant bacterial infections, and methods for treating such infections using such compounds and/or compositions. The invention includes administering an effective amount of a carbapenem compound or salt and/or prodrug thereof to a host in need of such a treatment.

专利号:US-8106031-B2
优先权日:2006-05-02
标题:Hydrolytically-resistant boron-containing therapeutics and methods of use
发明人：LEE VING; PLATTNER JACOB J; BENKOVIC STEPHEN J; BAKER STEPHEN J; MAPLES KIRK R; BELLINGER-KAWAHARA CAROLYN; AKAMA TSUTOMU; ZHANG YONG-KANG; SINGH RAJESHWAR; SAURO VITTORIO A
权利人:LEE VING; PLATTNER JACOB J; BENKOVIC STEPHEN J; BAKER STEPHEN J; MAPLES KIRK R; BELLINGER-KAWAHARA CAROLYN; AKAMA TSUTOMU; ZHANG YONG-KANG; SINGH RAJESHWAR; SAURO VITTORIO A; ANACOR PHARMACEUTICALS INC
摘要:Compositions and methods of use of boron derivatives, including benzoxaboroles, benzazaboroles and benzthiaboroles, as therapeutic agents for treatment of diseases caused by fungi, yeast, bacteria or viruses are disclosed, as well as methods for synthesis of said agents and compositions thereof.

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).