Synthesis of lanosterol derivatives with a functional group at C-32, including an antineoplastic sterol, 3 beta-hydroxylanost-7-en-32-oic acid

Lanosterol derivatives with a functional group at C-32 have been synthesized from 3 beta-acetoxylanostan-7 alpha-ol. The key reaction of the synthesis is the hypoiodite reaction of 3 beta-acetoxylanostan-7 alpha-ol. In vitro antitumor activity testing of the lanosterol derivatives revealed that 3 beta-hydroxylanost-7-en-32-oic acid has antineoplastic activity.     

A Simple Chaotic Circuit with Impulsive Switch Depending on Time and State

This paper presents a simple chaotic circuit consisting of two capacitors, one linear two-port VCCS and one time-state-controlled impulsive switch. The impulsive switch causes rich chaotic and periodic behavior. The circuit dynamics can be simplified into a one-dimensional return map that is piecewise linear and piecewise monotone. Using the return map, we clarify parameter conditions for existence of chaotic and periodic attractors and coexistence state of attractors.     

Energy storage in Ce-doped LiCaAlF6 and LiSrAlF6 crystals

Absorption, emission and thermoluminescence (TL) of as-grown and X-irradiated pure and Ce-doped LiCaAlF₆ (LiCAF) and LiSrAlF₆ (LiSAF) crystals have been analyzed. It is shown that the energy storage is defined by the dissimilarity of basic matrix properties, intrinsic defect structure, preferred Ce³⁺ ion disposition and charge compensation defect type. This is the reason of higher colorability and TL efficiency of as-grown Ce:LiSAF compared to Ce:LiCAF. Pre-filling of ultra-deep traps leads to enormous increases in the TL response. Due to these properties Ce:LiSAF and Ce:LiCAF are promising thermoluminescent dosimetric materials.     

Diversification of shotgun process

Three protocols for shotgun process are put forth in which simultaneous multi-fold reactions occur exclusively to each other. The first one involves simple combination of selective and non-selective reactions. Even if the simple protocol fails to give rise to the high selectivity, satisfactory outcome can be achieved by kinetic control or adjustment of functional groups.     

Effect of nitriding on grain oriented silicon steel bearing aluminum (the second study)

All kinds of high-permeability GO are manufactured using AlN as the main inhibitor. From a purely metallurgical viewpoint, three types of inhibitor preparation for high-permeability GO have been shown. They include a complete solution without nitriding, a complete precipitation with nitriding and a partial precipitation with nitriding. In this study, another possibility, i.e., a complete solution method with nitriding, was investigated to avoid the extra high-temperature slab reheating and to examine the effect of nitriding on GO bearing Al. This method can also provide the sharp Goss texture, and nitriding is shown to be very useful for changing the inhibitor intensity, depending on the primary grain size.     

Effects of natural polysaccharide addition on drug release from calcium-induced alginate gel beads

Calcium-induced alginate gel beads (Alg-Ca) containing various polysaccharides, including an alginate hydrolysate, were prepared and the drug release profiles were investigated. Hydrocortisone (HC) was gradually released from Alg-Ca into the mimic gastric fluid, while in intestinal fluid, it was quickly released with the dissolution of Alg-Ca. However, with Alg-Ca containing 5% chitin (CT), dissolution of Alg-Ca was not observed, and release of HC showed apparent zero-order kinetics. Furthermore, addition of the alginate hydrolysate altered the HC-release profile for Alg-Ca.     

One-step synthesis of 4-aminodihydrobenzofurans and 4-hydroxyindoles via dehydrogenation-heteromercuration of 2-alyl-3-aminocyclohexenones using mercury(II) acetate

On treatment of the 2-allyl-3-aminocyclohexenones with mercury(II) acetate, either sequence, dehydrogenation—oxymercuration or dehydrogenation—aminomercuration, occurred depending on the nature of the amino group in the substrate to yield the dihydrobenzofurans or indoles, respectively.     

Electron-transfer reactions and functionalization of cytochrome P450cam monooxygenase system in reverse micelles

Enzyme-based electron-transfer reactions involved in the cytochrome P450 monooxygenase system were investigated in nanostructural reverse micelles. A bacterial flavoprotein, putidaredoxin reductase (PdR), was activated and shown to be capable of catalyzing the electron transport from NADH to electron-carrier proteins such as cytochrome b5 (tCyt-b5) and putidaredoxin (Pdx) in reverse micelles. Ferric tCyt-b5 in reverse micelles was effectively converted to its ferrous form by the exogenous addition of separately prepared reverse micellar solution harboring PdR and NADH. The fact that direct interactions of macromolecular proteins should be possible in the reverse micellar system encouraged us to functionalize a multicomponent monooxygenase system composed of the bacterial cytochrome P450cam (P450cam), putidaredoxin (Pdx), and PdR in reverse micelles. The successful camphor hydroxylation reaction catalyzed by P450cam was significantly dependent on the coexistence of Pdx, PdR, and NADH but not H2O2, suggesting that the oxygen-transfer reactions proceeded via a "monooxygenation" mechanism. This is the first report of a multicomponent cytochrome P450 system exhibiting enzymatic activity in organic media.     

Scale-up of high shear granulation based on the internal stress measurement

Scale-up of wet granulation in a vertical high shear mixer was conducted. Pharmaceutical excipient powders composed of lactose, cornstarch and micro-crystallinecellulose, and hydroxypropylcellulose as a binder were mixed together and then granulated with purified water under various operating conditions and vessel scales. A novel internal stress measurement system was developed and stress of normal and tangential directions that granules received from the agitator blade during the granulation was continuously measured. The results indicated that granules received stress mainly from the tangential direction, which also showed the largest value near at the vessel wall. The effects of the agitator tip speed and the centrifugal acceleration on the measured stress was investigated. It was found that the tip speed of the agitator blade could be the main factor for the granule growth. The physical properties such as strength, size distribution and compressibility of granules prepared by changing the operating conditions and the vessel scales were evaluated and the scale-up characteristics of high shear granulation were investigated experimentally. The results showed that these physical properties had linear correlations with the tip speed. It was finally concluded that the scale-up of high shear granulation could be well conducted by means of the tip speed of the agitator blade.     

Facile construction and divergent transformation of polycyclic isoxazoles: direct access to polyketide architectures

[reaction: see text] Base-promoted cyclocondensation of C-chloro oximes with cyclic 1,3-diketones affords functionalized isoxazoles in good yield and under convenient reaction conditions. This process enables the synthesis of highly substituted products with notable functional group tolerance. The products obtained are directly converted to a variety of polyketide-derived polycyclic structures including xanthenes, anthracenes, and benzophenones.