Synthesis and Application of a New Fluorous-Tagged Ammonia Equivalent
作者:Simon D. Nielsen、Garrick Smith、Mikael Begtrup、Jesper L. Kristensen
DOI:10.1002/chem.200903178
日期:2010.4.19
A novel fluorous‐tagged ammoniaequivalent has been developed. It is based on a nitrogen–oxygen bond, which can be cleaved in a traceless manner by a molybdenum complex or samarium diiodide. The application in the synthesis of ureas, amides, sulfonamides, and carbamates is described. The scope of the fluorous NO linker is exemplified by the synthesis of itopride, a drug used for the treatment of functional
Cyclopentyl ethers and their preparation and pharmaceutical formulation
申请人:GLAXO GROUP LIMITED
公开号:EP0361772A2
公开(公告)日:1990-04-04
Compounds of the general formula (I)
and the physiologically acceptable solvates and cyclodextrin complexes thereof, in which
R¹ represents phenyl substituted by a group -NHCOR⁵ (where R5 is substituted phenyl);
A is -(CH₂)nX(CH₂)m- or -(CH₂)pS(O)q(CH₂)r- (where n is 1 or 2, m is 2-5 and X is cis or trans -CH=CH- or -CH₂CH₂- or m is 1-4 and X is -CH=C=CH-; p is 1-4, q is zero, 1 or 2 and r is 1-4);
Y is substituted or unsubstituted 3-phenoxy-2-hydroxypropyl.
These compounds inhibit gastric acid secretion and provide gastrointestinal cytoprotection and may be formulated for use in the treatment of ulcers. They may also be of use in the therapy or prophylaxis of atherosclerosis and other disorders associated with abnormal levels of blood lipids and serum chlolesterol.
通式(I)化合物
及其生理学上可接受的溶解物和环糊精络合物,其中
R¹ 代表被基团 -NHCOR⁵ 取代的苯基(其中 R5 为取代的苯基);
A 是-(CH₂)nX(CH₂)m- 或-(CH₂)pS(O)q(CH₂)r-(其中 n 是 1 或 2,m 是 2-5,X 是顺式或反式-CH=CH- 或-CH₂CH₂-,或 m 是 1-4,X 是-CH=C=CH-;p 是 1-4,q 是零、1 或 2,r 是 1-4);
Y 是取代或未取代的 3-苯氧基-2-羟基丙基。
这些化合物可抑制胃酸分泌,提供胃肠道细胞保护,可配制成治疗溃疡的药物。它们还可用于治疗或预防动脉粥样硬化和其他与血脂和血清胆固醇水平异常有关的疾病。
Gold-Catalyzed Hydration of Haloalkynes to α-Halomethyl Ketones
作者:Longyong Xie、Yundong Wu、Weiguo Yi、Lei Zhu、Jiannan Xiang、Weimin He
DOI:10.1021/jo401437w
日期:2013.9.20
A general atom-economical approach for the synthesis of alpha-halomethyl ketones is demonstrated through hydration of a wide range of haloalkynes. Other outstanding features include excellent yields from both alkyl- and aryl-substituted haloalkynes and wide functional group tolerance. This protocol is an alternative to conventional alpha-halogenation of ketones.
Mild chemo-selective hydration of terminal alkynes catalysed by AgSbF<sub>6</sub>
作者:Mathieu Bui The Thuong、André Mann、Alain Wagner
DOI:10.1039/c1cc12928g
日期:——
The chemo-selective hydration of a wide range of non-activated terminal alkynes catalysed by AgSbF6 under mild conditions is reported.