Recent Disclosures

Several series of CCR5 antagonists have been disclosed in the journal and patent literature, for which there is little detail available. 

Kemia have disclosed a series of bis-aniline urea-based derivatives of the Pfizer tropane series induding 31 which showed good antiviral activity HIV-1 (EC90 6nM) and encouraging pharmacokinetics in the rat P 52%, To.s 7.2 h) [126]. 

Examples of other series recently disdosed in the patent literature are shown below in structures 33-37 [125-128]. 

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Due to its broad scope, as well as to its favorable features (commercial availability of the catalyst, use of a "green" oxidant, economy, extremely simple procedure and work-up), this method has been rapidly accepted, as demonstrated by its use by several different research groups, despite its recent disclosure.1617 This procedure employing CH3Re03 and UHP appears to be the method of choice when optically active nitrones are prepared by oxidation of the corresponding amines.14 15 18... 

A series of 2-amino-3/4-dihydro quinazolines have been extensively explored as selective T-type calcium channel antagonists. A recent disclosure included KYS05090 (9) with an IC50 of 41 nM on the Cav3.1 subtype of the T-type channel and 120-fold selectivity versus the N-type calcium channel Cav2.2 [55]. A pharmacophore model was recently published based on this and related structures [56], but no other selectivity or in vivo activity have been disclosed since the original report. 

The recent disclosure of 21 (S/GSK1349572) as a next generation INI has been supported by preclinical data showing this compound to be a potent antiviral (PBMC IC50 = 0.15 ng/mL) with a low clearance and good oral bioavailability Cl, (%F) across species (rat 0.2mL/min/kg, (35%), dog 2.2, (35%), cyno 2.1, (25%)) [56]. The protein-binding-adjusted... 

The relative value of n-butyraldehyde and isobutyraldehyde is well exemplified by the recent disclosure (33) of a process for decomposing unwanted isobutyraldehyde back to the elements of propylene, carbon monoxide, and hydrogen for recycling to make more n-butyraldehyde. 

Another recent disclosure examined silicon-to-copper transmetallation as a mild means of synthesizing alkenyl-copper reagents from stable precursors. The method requires activation of the silyl group by an allylic alcohol. Again, the silanes in this work are produced by circuitous means but should be accessible by ruthenium-catalyzed hydrosilylation. Treatment of the silyl alcohol with a stoichiometric amount of copper(l) /rz -butoxide results in the C-to-O migration of the silyl group to produce a vinylcuprate shown to be competent for subsequent allylation to produce 1,4-diene products (Scheme 17). 

Finally, in a very recent disclosure, Lee et al. (165) approached the total synthesis of arteminolide using a [5 + 2] cycloaddition strategy with an oxidopyrylium ion. Despite its long history of use, Lee was the first to utilize an allene moiety both in an intra- and an intermolecular cycloaddition with oxidopyrylium ions. By utilizing a pyrone cycloaddition precursor (294) similar to those used in the Wender phorbol synthesis, Lee was able to synthesize various ring sizes and... 

Attention may be drawn, finally, to recent disclosure that a J0-rpoxy ketones aro converted to the corresponded allyEc abobola on... 

Moreover, the use of PB will not only be limited to the detection of H202 and its use in conjunction with oxidase enzymes. A recent disclosure of the electrocatalytic activity of PB towards the oxidation of thiols will also be discussed and an application with acetylcholinesterase enzymes for pesticide detection reported. 

The content of this book reviews the latest developments in the characterization and chemical modification of silica surfaces. No attempt has been made to survey exhaustively the literature of any topic. The material has been collected from recent publications and own research work in this field. Also, recent disclosures of research activities in the former USSR are documented in detail in the text. 

Although our initial concerns about possible interferences due to chemiluminescence and quenching effects have been somewhat mitigated by recent disclosures of Blank and Kidwell s tritium counting procedures, an entirely different problem exists concerning their isotopic method, one that in our opinion casts serious doubt upon the general suitability of their approach for doing hair contamination/decontamination studies. 

A wide range of hetero 2-aza-1,3-butadienes have been shown to participate as 4rr components of Diels-Alder reactions (Figure 4). Perhaps the most widely recognized class of hetero 2-aza-1,3-butadienes is the A -acylimines (l-oxa-3-aza-l,3-butadiene) ° and comprehensive reviews of their 4tt participation in LUMOdiene-controlled Diels-Alder reactions are available. The recent disclosure of the 4ir participation of A -acylimines in intramolecular [4 + 2] cycloaddition reactions (equation 11), and the use of optically active A -acylimines in productive LUMOdiene-controlled [4 + 2] cycloaddition reactions, illustrate applications of the systems that have not been explored fully (equation 12). ... 

This article summarizes recent advances in the synthesis of natural products by hetero Diels-Alder cycloaddition reactions up to 1985. These recent disclosures have had a great impact on heterocyclic natural product syntheses. 

A recent disclosure by Helmchen has demonstrated that (phosphino-oxazo-line)copper(II) complexes are also good chiral templates for asymmetric cataly-... 

Note added to proof The recent disclosure by Mobil Scientists (36) of a new family of highly uniform mesoporous silicas is of great potential significance. One member, MCM-41, has been shown (P. J. Branton, P. G. Hall, K. S. W. Sing, unpublished work) to give a reversible Type IV nitrogen isotherm and to possess a very narrow range of pores. 

In response to these concerns, and particularly the ones associated with tire nonabsorbable cyanoacrylates that are used clinically. Linden and Shalaby disclosed a novel, absorbable tissue adhesive composition that addressed, to a practical extent, the drawbacks of the absorbable bioadhesive as well as nonabsorbable cyanoacrylates. In effect, these absorbable tissue adhesive compositions were based (1) primarily on methoxyalkyl cyanoacrylates and preferably methoxypropyl cyanoacrylate as the precursor of an absorbable tissue adhesive polymer and (2) on a polymeric, highly absorbable, liquid comprising an oxalate ester of triethylene glycol as a modifier to modulate the viscosity of the overall composition, lower the heat of polymerization, and increase the compliance and absorption rate of the cured adhesive joint. In a more recent disclosure by Shalaby, a number of other useful modifiers were described and the functional performance of the new adhesive compositions was reported. ... 

Allylamines have received much attention in the recent literature, a trend which appears to be continuing. a-sec-Allylamines have been rarely reported but a recent disclosure describes their syn-thesis via application of the Bruylants reaction. The method is versatile in that either enals can be converted to vinyl amino-nitriles prior to reaction with a Grignard reagent, or vinyl Grignard reagents can be reacted with a-aminonitriles (Scheme 15). Yields of the products were moderate to good. 

The precise function of microfibrils in hard elastic polymers is not well understood. Their importance in various models of crystalline polymers has ranged from mere tie points [4,5] to the fundamental element [9]. The recent disclosure of hard elastic behavior in crazed HIPS [11] clearly revealed the connection between microfibrillar superstructure and hard elastic behavior, since no lamellae exists in this material. Polymers with a fibrillar structure are not necessarily hard elastic,however. Gore-Tex has an extensive fibrillar domain as shown in Figure 2c. Its loading cycle (Figure 5), however, clearly reveals an inelastic material. Hence, the necessary criterion of microfibrillar structure for a hard elastic polymer must be established. 

Following their recent disclosure of a three-step process for the replacement of oxygen in ketones by two methyl groups, Reetz and his co-workers have now... 

Recent disclosures about the electrical conduction properties of various poly(arylamines), many of which contain condensed aromatic kernels [511-513], will undoubtedly increase the interest in this family of aromatic networks with unusual electric and magnetic properties. A brief review describing some of the above and other polymers with potentially interesting magnetic properties recently appeared in the open literature [514]. 

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