54150-57-1Relevant academic research and scientific papers
Decarboxylative Synthesis of Functionalized Oxindoles via An Iron-Initiated Radical Chain Process and Application in Constructing Diverse Fused-Indoline Heterocycles
Cui, Zhihao,Du, Da-Ming
supporting information, p. 93 - 99 (2017/10/24)
Rapid construction of diverse fused-indoline?heterocycle (FIH) frameworks including high-value pyrroloindolines, furoindolines and thienoindolines in a two-step sequence has been described. The key to success hinges on the adoption of peresters as α-heteroatom alkyl radical precusors, which can smoothly react with N-arylacrylamides via a radical chain process initiated by inexpensive FeCl2?4H2O to afford the functionalized oxindoles, the key intermediates to FIH skeletons. The approach features operationally-simplicity, broad substrates scope and mild conditions. (Figure presented.).
Prodrug derivatives of carboxylic acid drugs
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, (2008/06/13)
Novel ester derivatives of carboxylic acid medicaments of formula (I), wherein R--COO--represents the acyloxy residue of a carboxylic acid drug or medicament, n is an integrer from 1 to 3, and R1 and R2 are the same or different and are selected from a group consisting of an alkyl, an alkenyl, an aryl, an aralkyl, a cycloalkyl and which group may be unsubstituted or substituted, or R1 and R2 together with the N forms a 4-, 5-, 6- or 7-membered heterocyclic ring, which in addition to the nitrogen atom may contain one or two further heteroatoms selected from the group consisting of nitrogen, oxygen and sulfur and which heterocyclic group may be substituted. These compounds are highly biolabile prodrug forms of the corresponding carboxylic acid compounds and are highly susceptible to undergoing enzymatic hydrolysis in vivo whereas they are highly stable in aqueous solution. The novel derivatives are less irritating to mucosa than the parent carboxylic acids and may provide an improved bio-availability of the drugs.
Glycolamide esters as biolabile prodrugs of carboxylic acid agents: synthesis, stability, bioconversion, and physicochemical properties.
Nielsen,Bundgaard
, p. 285 - 298 (2007/10/02)
Benzoic acid esters of various substituted 2-hydroxyacetamides (glycolamides) were found to be hydrolyzed extremely rapidly in human plasma solutions, the half-lives of hydrolysis being less than 5 s in 50% plasma solutions for some N,N-disubstituted glycolamide esters. The rapid rate of hydrolysis could be largely attributed to cholinesterase (also called pseudocholinesterase) present in plasma. From a study of a variety of substituted glycolamide esters and structurally related esters, the most prominent structural requirement needed for a rapid rate of hydrolysis was found to be the glycolamide ester structure combined with the presence of two substituents on the amide nitrogen atom. A structural similarity of such esters with benzoylcholine, a good substrate for cholinesterase, was put forward. Esters of N,N-disubstituted glycolamides are suggested to be a useful biolabile prodrug type for several carboxylic acid agents. The esters combine a high susceptibility to undergo enzymatic hydrolysis in plasma with a high stability in aqueous solution. Furthermore, as demonstrated with the benzoic acid model esters, it is feasible to obtain ester derivatives with almost any desired water solubility or lipophilicity with retainment of marked lability to enzymatic hydrolysis.
Glycolate ester peracid precursors
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, (2008/06/13)
The invention provides novel bleaching compositions comprising peracid precursors with the general structure STR1 with R, R', R" and L as defined in the specification. Novel peracids and precursors are also herein disclosed. These peracid precursors provide new, proficient and cost-effective compounds for fabric bleaching.
Total Synthesis of (+/-)-3-Deoxy-D-manno-2-octulopyranosonate (KDO)
Danishefsky, Samuel J.,Pearson, William H.,Segmuller, Brigitte E.
, p. 1280 - 1285 (2007/10/02)
Cyclocondensation of 2-(phenylseleno)propionaldehyde with 1-(α-furyl)-1-methoxy-3--4-(benzoyloxy)-1,3-butadiene under the influence of boron trifluoride produces a predominance (2.4:1) of cis-/trans-3-(benzoyloxy)-6-(α-furyl)-2-(1-ph
Hydroxyaminohydrocarbonphosphonic acids
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, (2008/06/13)
New hydroxyaminohydrocarbonphosphonic acid derivatives of the formula: STR1 wherein R1 is hydrogen or acyl, R2 is hydrogen, lower alkyl, ar(lower)alkyl or acyl, and A is lower alkylene, lower alkenylene or hydroxy(lower)alkylene, or
