143761-23-3Relevant academic research and scientific papers
Regio-selective reduction of the C-C double bonds in α,β- unsaturated acyl 4-substituted oxazolidin-2-ones and oxazolidine-2-thiones
Li, Shao-Gang,Jin, Jian-Wei,Wu, Yikang
, p. 846 - 850 (2012/02/02)
Selective saturation of the conjugated C-C double bonds in the title compounds was examined in a systematic way for the first time. Many established protocols effective for similar reduction of α,β-unsaturated ketones and esters in the literature were found to be inapplicable in the present context. The most satisfactory results were finally obtained using the DIBAL-H/MeLi/CuI/HMPA/THF conditions.
Total synthesis of 26-fluoro-epothilone B
Koch, Guido,Loiseleur, Olivier,Altmann, Karl-Heinz
, p. 693 - 697 (2007/10/03)
An efficient synthesis of the epothilone B derivative 26-fluoroepothilone B (1) was realized by early introduction of the synthetically demanding fluoromethyl epoxide function. The presence of a fluoro substituent results in a remarkable increase in the stability of the epoxide, which tolerates the wide range of reaction conditions required for the fragment coupling step and end game transformations.
A NEW PROCESS FOR THE PREPARATION OF EPOTHILONE DERIVATIVES, NEW EPOTHILONE DERIVATIVES AS WELL AS NEW INTERMEDIATE PRODUCTS FOR THE PROCESS AND THE METHODS OF PREPARING SAME
-
Page 20, (2008/06/13)
The present invention provides a synthesis for the preparation of epothilone derivatives of formula (9) wherein R1 is methyl, and R2 has the meaning of an unsubstituted or substituted aryl, an unsubstituted or substituted heteroaryl or an unsubstituted or substituted heterocyclic radical fused to a benzene nucleus, and salts thereof, and intermediates for the synthesis of a compound of formula (9).
The design, synthesis, and structure-activity relationships of a series of macrocyclic MMP inhibitors
Steinman, Douglas H.,Curtin, Michael L.,Garland, Robert B.,Davidsen, Steven K.,Heyman, H. Robin,Holms, James H.,Albert, Daniel H.,Magoc, Terry J.,Nagy, Ildiko B.,Marcotte, Patrick A.,Li, Junling,Morgan, Douglas W.,Hutchins, Charles,Summers, James B.
, p. 2087 - 2092 (2007/10/03)
A series of succinate-derived hydroxamic acids incorporating a macrocyclic ring were designed, synthesized, and evaluated as inhibitors of matrix metalloproteinases. The inhibitors were designed based on the published X-ray crystal structure of batimastat (1) complexed with human neutrophil collagenase (MMP-8). The synthesized compounds were shown to inhibit selected MMPs in vitro with low nanomolar potency.
Inhibition of matrix metalloproteinases by hydroxamates containing heteroatom-based modifications of the P1' group
Gowravaram,Tomczuk,Johnson,Delecki,Cook,Ghose,Mathiowetz,Spurlino,Rubin,Smith,Pulvino,Wahl
, p. 2570 - 2581 (2007/10/02)
In this study, structure-based drug design of matrix metalloproteinase inhibitors [human fibroblast collagenase (HFC), human fibroblast stromelysin (HFS), and human neutrophil collagenase (HNC)] was utilized in the development of potent hydroxamates which
Thromboxane Receptor Antagonism Combined with Thromboxane Synthase Inhibition. 5. Synthesis and Evaluation of Enantiomers of 8-amino>-4-(3-pyridinylalkyl)octanoic Acid
Bhagwat, Shripad S.,Gude, Candido,Cohen, David S.,Dotson, Ron,Mathis, Janice,et al.
, p. 205 - 210 (2007/10/02)
The enantiomers of 8-amino>-4-(3-pyridinylpropyl)octanoic acid (1) and its pyridinyl ether analog (2) were synthesized using the highly diastereoselective method of alkylation of acyloxazolidinone.These enantiomerically pure com
CERTAIN (ARYLSULFONAMIDO- AND IMIDAZOLYL-)-SUBSTITUTED CARBOXYLIC ACIDS AND DERIVATIVES THEREOF AND USE FOR SUPPRESSING THROMBOXANE ACTIVITY
-
, (2008/06/13)
The present invention is concerned with compounds of formula I STR1 wherein A, B, M, R, Ar and Het are as defined in the specification, pharmaceutically acceptable ester and amide derivatives thereof; N-oxides thereof, tetrazole derivatives thereof, and s
