Methods For Preparing Fluoroalkyl Arylsulfinyl Compounds And Fluorinated Compounds Thereto
申请人:Umemoto Teruo
公开号:US20110190511A1
公开(公告)日:2011-08-04
Novel preparative methods for fluoroalkyl arylsulfinyl compounds are disclosed. Fluorinated compounds as useful fluorinated compounds, intermediates, or builing blocks are disclosed. Useful applications of the fluoroalkyl arylsulfinyl compounds are shown.
Methods for Preparing Fluoroalkyl Arylsulfinyl Compounds and Fluorinated Compounds Thereto
申请人:Umemoto Teruo
公开号:US20100152463A1
公开(公告)日:2010-06-17
Novel preparative methods for fluoroalkyl arylsulfinyl compounds are disclosed. Fluorinated compounds as useful fluorinated compounds, intermediates, or building blocks are disclosed. Useful applications of the fluoroalkyl arylsulfinyl compounds are shown.
7β-Acylamino-3-alkoxycarbonyl-(and 3-keto)-1-carba (1-dethia)-3-cephem-4-carboxylic acids and derivatives and related 3-substituted compounds are provided as antibiotics useful for treating infections in man and other animals. Pharmaceutical formulations comprising the antibiotics, intermediates, and a process for their preparation are also provided.
Gemcitabine prodrugs, pharmaceutical compositions and uses thereof
申请人:——
公开号:US20040142857A1
公开(公告)日:2004-07-22
The present invention provides gemcitabine prodrugs, methods of making gemcitabine prodrugs, pharmaceutical compositions of gemcitabine prodrugs and methods of using gemcitabine prodrugs and pharmaceutical compositions thereof to treat or prevent diseases or disorders such as cancer or viral infections.
Aminolyses of 4-Nitrophenyl Phenyl Carbonate and Thionocarbonate: Effect of Modification of Electrophilic Center from CO to CS on Reactivity and Mechanism
作者:Ik-Hwan Um、Eun Young Kim、Hye-Ran Park、Sang-Eun Jeon
DOI:10.1021/jo052417z
日期:2006.3.1
[GRAPHICS]A kinetic study is reported for nucleophilic substitution reactions of 4-nitrophenyl phenyl carbonate (5) and 4-nitrophenyl phenyl thionocarbonate (6) with a series of primary amines. The thiono compound 6 is less reactive than its oxygen analogue 5 toward strongly basic amines but is more reactive toward weakly basic CF3CH2NH2. The Bronsted-type plots obtained from the aminolyses of 5 and 6 are curved downwardly. The reactions are proposed to proceed through a stepwise mechanism with a change in the RDS on the basis of the curved Bronsted-type plots. The microscopic rate constants (k(1) and k(2)/k(-1) ratio) associated with the current aminolyses are consistent with the proposed reaction mechanism. The replacement of the C=O bond in 5 by a polarizable C=S group results in a decrease in the k(1) value but an increase in the k(2)/k(-1) ratio. Besides, such a modification of the electrophilic center causes a decrease in pK(a)degrees, defined as the pK(a) at the curvature center of curved Bronsted-type plots, but does not alter the reaction mechanism. The larger k(2)/k(-1) ratio for the reactions of 6 compared to those of 5 is proposed to be responsible for the decreased pK(a)degrees value.