13605-66-8Relevant academic research and scientific papers
High catalytic activity of a new Ag phosphorus ylide complex supported on montmorillonite: synthesis, characterization, and application for room temperature nitro reduction
Karami, Kazem,Rahimi, Mahzad,Dinari, Mohammad
, p. 281 - 291 (2018)
In this work, the phosphorus ylide, [PPh3CHC(O)CH2Cl], was reacted with AgNO3 to give the [Ag{C(H)PPh3C(O)CH2Cl}2]+NO3? as the product. Then, it was supported on the modified montmorillonite nanoclay to prepare a new catalyst for the reduction reaction. The structure and morphology of the nanoclay catalyst were characterized by FT-IR, X-ray powder diffraction, scanning electron microscopy, energy-dispersive X-ray analysis and transmission electron microscopy techniques; also, the content of silver was obtained by inductively coupled plasma analyzer. This composition was exploited to study its catalytic activity in the reduction in aromatic nitro compounds; it displayed the high catalytic activity. Factors such as catalyst amount, solvent, temperature and reaction time were all systematically investigated to elucidate their effects on the yield of catalytic reduction in nitroarenes. This catalytic system exhibited high activity toward aromatic nitro compounds under mild conditions. The catalyst was reused five times without any significant loss in its catalytic activity.
Preparation and biological evaluation of BACE1 inhibitors: Leveraging trans-cyclopropyl moieties as ligand efficient conformational constraints
Audia, James E.,Barberis, Mario,Beck, James P.,Boggs, Leonard N.,Borders, Anthony R.,Boyer, Robert D.,Brier, Richard A.,Erickson, Jon A.,Garcia-Losada, Pablo,Green, Steven J.,Hembre, Erik J.,Hendle, J?rg,Lopez, Jose E.,Mathes, Brian M.,May, Patrick C.,Mergott, Dustin J.,Minguez, Jose Miguel,Monk, Scott A.,Porter, Warren J.,Rankovic, Zoran,Shi, Yuan,Stout, Stephanie L.,Timm, David E.,Watson, Brian M.,Winneroski, Leonard L.,Yang, Zhixiang
, (2019)
Inhibition of BACE1 has become an important strategy in the quest for disease modifying agents to slow the progression of Alzheimer's disease. We previously reported the fragment-based discovery of LY2811376, the first BACE1 inhibitor reported to demonstrate robust reduction of human CSF Aβ in a Phase I clinical trial. We also reported on the discovery of LY2886721, a potent BACE1 inhibitor that reached phase 2 clinical trials. Herein we describe the preparation and structure activity relationships (SAR) of a series of BACE1 inhibitors utilizing trans-cyclopropyl moieties as conformational constraints. The design, details of the stereochemically complex organic synthesis, and biological activity of these BACE1 inhibitors is described.
FLUORESCENT SYSTEMS FOR BIOLOGICAL IMAGING AND USES THEREOF
-
, (2021/02/12)
The invention relates to compounds of formula I, in which Y, Ar1, Ar2, X, R1 and R2 are defined herein, and to their use in a variety of biological imaging techniques and therapeutic methods. In aspects, the invention relates to conjugates comprising the compounds of formula I and their associated uses and therapeutic uses.
AZEPANE DERIVATIVES AND METHODS OF TREATING HEPATITIS B INFECTIONS
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, (2015/07/22)
Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
AZEPANE DERIVATIVES AND METHODS OF TREATING HEPATITIS B INFECTIONS
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Paragraph 0550, (2015/09/22)
Provided herein are compounds useful for the treatment of HBV infection in a subject in need thereof, pharmaceutical compositions thereof, and methods of inhibiting, suppressing, or preventing HBV infection in the subject.
One-pot eschenmoser episulfide contractions in DMSO: Applications to the synthesis of fuligocandins A and B and a number of vinylogous amides
Pettersson, Birgitta,Hasimbegovic, Vedran,Bergman, Jan
, p. 1554 - 1561 (2011/05/19)
Practical total syntheses of the natural products fuligocandin A (2a) and fuligocandin B (3) have been achieved through a convergent strategy depending on the Eschenmoser episulfide contraction as a key step. Conducting the reaction in DMSO proved to be an efficient and general method for the synthesis of a variety of vinylogous amides, such as azepan-2- ylidenepropan-2-one. 2011 American Chemical Society.
Total synthesis of fuligocandines A and B
Pettersson, Birgitta,Hasimbegovic, Vedran,Bergman, Jan
scheme or table, p. 238 - 239 (2010/03/24)
A practical synthesis of the biologically active cycloanthranilylproline derivatives fuligocandines A and B is described, starting from l-proline and isatoic anhydride, employing an Eschenmoser episulfide contraction as the key step.
A convergent total synthesis of (+)-febrifugine
Sieng, Bora,Ventura, Oscar Lozano,Bellosta, Véronique,Cossy, Janine
scheme or table, p. 1216 - 1218 (2009/04/04)
Febrifugine was synthesized in ten steps from N-Boc 4-aminobutan-1-ol by a convergent approach. Georg Thieme Verlag Stuttgart.
New nitrogenated siloxy butadienes from 1,3-dichloroacetone
Alonso, Dulce,Caballero, Esther,Medarde, Manuel,Tomé, Fernando
, p. 907 - 910 (2008/02/03)
New 1-formamido-2-siloxy-1,3-butadienes have been generated from 1,3-dichloroacetone by means of phosphorane formation, formamido substitution, Wittig olefination and silylation. The procedure demonstrates the utility and versatility of this methodology for the formation of polysubstituted dienes, designed as useful building blocks for the synthesis of polycyclic alkaloids and related analogues.
Synthesis of 3-oxooxa- and 3-oxoazacycloalk-4-enes by ring-closing metathesis. Application to the synthesis of an inhibitor of cathepsin K
Taillier, Catherine,Hameury, Thomas,Bellosta, Véronique,Cossy, Janine
, p. 4472 - 4490 (2008/02/01)
3-Oxooxa- and 3-oxoazacycloalk-4-enes were obtained with good yield from 1-(ω-alkenyloxy)- and 1-(ω-alkenylamino)-but-3-en-2-ones by using a ring-closing metathesis. This methodology has been used to synthesize an inhibitor of cathepsin K.
