CAS: 26394-17-2; Cyclopentanesulfonylchloride

相似化合物

1955560-75-4 1512580-62-9 242459-85-4

📜环戊硫醇置于过氧乙酸,氯化亚砜,溶剂黄146体系中,化学反应 6.0H,反应生成环戊烷磺酰氯
参考文献:具有有效的体内功效的有效和选择性的基于2-氨基苯并咪唑的p38Alpha Map激酶抑制剂的设计.
标题:具有有效的体内功效的有效和选择性的基于2-氨基苯并咪唑的p38Alpha Map激酶抑制剂的设计.
摘要:我们报告了基于2-氨基苯并咪唑的有效和高度选择性的p38Alphainhibitors系列的设计和发现.铅化合物1在atp竞争性酶结合和巨噬细胞中的tnfα释放抑制方面均具有低纳摩尔活性.与其他p38参考化合物相比,化合物18在大鼠胶原蛋白诱发的关节炎模型中显示出出色的药代动力学特性和口服活性.还介绍了解决cyp3A4责任的sar策略.
Doi:10.1021/jm048978K

专利信息

专利号:US-6639059-B1
优先权日:1999-03-24
标 题 :Synthesis of [2.2.1]bicyclo nucleosides
发明人：KOCHKINE ALEXEI; FENSHOLDT JEF; PFUNDHELLER HENRIK M
权利人:EXIQON AS
摘要:A synthesis of [2.2.1]bicyclo nucleosides which is shorter and provides higher overall yields proceeds via the key intermediate of the general formula III, wherein R4 and R5 are, for instance, sulfonates and R7 is, for instance, a halogen or an acetate. From compounds of the general formula II, such as 3-O-aryl-4-C-hydroxymethyl-1,2-O-isopropylidene-alpha-D-ribofuranose, intermediates of the general formula III are suitable for coupling with silylated nucleobases. Upon one-pot base-induced ring-closure and desulfonation of the formed [2.2.1]bicyclo nucleoside, a short route to each the LNA (Locked Nucleic Acid) derivatives of adenosine, cytosine, uridine, thymidine and guanidine is demonstrated. The use of the 5'-sulfonated ring-closed intermediate also allows for synthesis of 5'-amino- and thio-LNAs.

专利号:US-6734291-B2
优先权日:1999-03-24
标题:Synthesis of [2.2.1]bicyclo nucleosides
发明人：KOCHKINE ALEXEI; FENSHOLDT JEF; PFUNDHELLER HENRIK M
权利人:EXIQON AS
摘要:A synthesis of [2.2.1]bicyclo nucleosides which is shorter and provides higher overall yields proceeds via the key intermediate of the general formula III, wherein R4 and R5 are, for instance, sulfonates and R7 is, for instance, a halogen or an acetate. From compounds of the general formula II, such as 3-O-aryl-4-C-hydroxymethyl-1,2-O-isopropylidene-alpha-D-ribofuranose, intermediates of the general formula III are suitable for coupling with silylated nucleobases. Upon one-pot base-induced ring-closure and desulfonation of the formed [2.2.1]bicyclo nucleoside, a short route to each the LNA (Locked Nucleic Acid) derivatives of adenosine, cytosine, uridine, thymidine and guanidine is demonstrated. The use of the 5'-sulfonated ring-closed intermediate also allows for synthesis of 5'-amino- and thio-LNAs

专利号:US-10125226-B2
优先权日:2013-06-05
标 题 :Scale-up process of bifunctionalized triblock copolymers with secondary and tertiary amines, with application in dewatering and desalting of heavy crude oils
发明人：FLORES SANDOVAL CESAR ANDRES; FLORES OROPEZA EUGENIO ALEJANDRO; LOPEZ ORTEGA ALFONSO; HERNANDEZ CORTEZ JOSE GONZALO; ESTRADA BUENDIA ARISTEO; CASTRO SOTELO LAURA VERONICA; REYES MARTINEZ REYNA; ALVAREZ RAMIREZ FERNANDO; ESTRADA MARTINEZ ARQUIMEDES; VAZQUEZ MORENO FLAVIO SALVADOR
权利人:MEXICANO INST PETROL
摘要:A chemical synthesis process is provided for the functionalization of monodispersed triblock copolymer (POEw-POPy-POEw) with secondary or tertiary amines at a semi-industrial level in glass reactors having a capacity between 1 L and 100 L. The process includes two stages where the first stage uses an alkylsulfonyl or arylsulfonyl chloride to obtain better leaving groups, and the second stage is the nucleophilic substitution with secondary or tertiary amines, to obtain the bifunctionalized triblock copolymers. The main advantage for this process is to reduce the quantity of unitary process done in each stage, the optimization of reaction times, and the stoichiometric relationships.

专利号:US-2003092905-A1
优先权日:1999-03-24
标 题:Synthesis of [2.2.1]bicyclo nucleosides

专利号:WO-2010115869-A1
优先权日:2009-04-03
标 题 :Propofol phosphonyl derivatives, synthesis, and use in long acting formulations
发明人：GONNISSEN YVES RENE JOHANNA PAUL
权利人:SEPS PHARMA N V; GONNISSEN YVES RENE JOHANNA PAUL
摘要:This invention relates to compounds represented by the structural formula (I), and the salts and stereoisomers thereof, wherein: - L is a linker selected from the group consisting of -(CH 2 ) P -O-, a single bond, formula (IA), -(CH 2 ) 1-8 -O-X(O)-, and - p is an integer from 1 to 8, - each R 3 and each R 4 is independently selected from the group consisting of C 1-20 alkyl, C 3-12 alkyl, C 3-12 cycloalkyl-C 1-4 alkyl, saturated heterocyclyl and saturated heterocyclyl-C 1-4 alkyl, and - X and Y are each independently C or S(O), - Z is selected from the group consisting of O, S(O) and NR 5 , - W is selected from the group consisting of halogen, OH, S(O)H and O - M + wherein M + is a monovalent cation; and - R 5 is selected from the group consisting of hydrogen and C 1-10 alkyl. These compounds are useful pharmaceutical agents with improved oral bioavailability.

专利号:WO-0056746-A2
优先权日:1999-03-24
标题 :Improved synthesis of [2.2.1]bicyclo nucleosides