Peptide late-stage C(sp3)–H arylation by native asparagine assistance without exogenous directing groups

There is a strong demand for novel native peptide motifs for post-synthetic modifications of peptides without pre-installation and subsequent removal of directing groups. Herein, we report an efficient method for peptide late-stage C(sp³)–H arylations assisted by the unmodified side chain of asparagine (Asn) without any exogenous directing group. Thereby, site-selective arylations of C(sp³)–H bonds at the N-terminus of di-, tri-, and tetrapeptides have been achieved. Likewise, we have constructed a key building block for accessing agouti-related protein (AGRP) active loop analogues in a concise manner.

An efficient method for peptide late-stage C(sp³)-H arylations assisted by unmodified side chain of asparagine (Asn) without any exogenous directing group has been reported.     

One-pot two-step microwave-assisted reaction in constructing 4,5-disubstituted pyrazolopyrimidines

[reaction: see text] A microwave-assisted reaction was developed to facilitate the construction of 4,5-disubstituted pyrazolopyrimidines. This one-pot two-step process involves a sequential S(N)Ar displacement of the C4 chloro substituent with various anilines and amines, followed by a Suzuki coupling reaction with different boronic acids. Using microwave irradiation leads to high product conversion, low side product formation, and shorter reactions.     

Microdialysis sampling coupled to HPLC for transdermal delivery study of ondansetron hydrochloride in rats

The transdermal delivery of ondansetron hydrochloride (ON) solution in propylene glycol (PG) with a widely used penetration enhancer, oleic acid (OA), was studied in rats by a microdialysis sampling technique. Dialysate samples collected from the probe were directly injected into the HPLC system without any pre-treatment and no interference occurred in the blank sample. A good linearity between the standard concentrations and peak areas within the calibration range was achieved. In vivo recovery (32.52 +/- 1.8%) of the probe was assessed with the retrodialysis method, which was used to calculate the ON concentration in the dermis. Oleic acid at the concentrations of 2% and 5% (w/v) increased the steady-state delivery rate from 0.001 to 0.030 and 0.058 microg/h, respectively. OA proved to be an effective enhancer for transdermal delivery of ON in rats.     

市场化改革背景下养老机构服务供给博弈研究

考虑政府补贴、市场化程度、养老机构服务成本、老年人偏好等因素,构建了完全国有化、公私并存的半市场化和完全市场化三种情形下公办和民办养老机构之间的两阶段博弈模型,比较分析了市场化程度对养老机构服务价格制定和服务水平选择的影响,实证讨论了各参数变化对养老机构收益及社会福利的影响。研究表明:完全市场化机制会降低养老机构服务质量,完全国有化机制会陷入社会福利陷阱,探索公私并存的最佳市场化水平才能更好地提高社会福利;适度推进市场化改革,提高养老机构服务水平,降低民办养老机构服务成本,适度提高对民办养老机构的补贴,将有效缓解公办和民办养老机构的不公平竞争;提高老年人支付能力,推进养老机构供给侧结构性改革,将保障机构养老服务的有效供给,促进养老服务业的健康有序发展。     

Characterizing the dynamics of auditory perception

After listening to a sound that is presented repeatedly, subjects report hearing different transforms of the original sound. The frequency of reported transforms is a sensitive index of some speech disorders as well as cognitive flexibility in aging. In this paper, we propose and investigate quantitative measures that characterize the dynamics of this phenomenon, known as the verbal transformation effect. In particular, we show that the distribution of the dwell time, the time spent perceiving a string of a given phonemic form before switching to another form, obeys a power law for normal subjects with an exponent valued between 1 and 2. This result suggests that within this paradigm there is no characteristic time scale for the perceptual process. Additionally, we analyze the correlation properties of the transforms. We suggest that the complexity measures and techniques introduced here might be useful diagnostic tools for a number of speech and cognitive disorders. (c) 1995 American Institute of Physics.     

The projection method for computing multidimensional absolutely continuous invariant measures

We present an algorithm for numerically computing an absolutely continuous invariant measure associated with a piecewiseC ² expanding mappingS: on a bounded region R ^N. The method is based on the Galerkin projection principle for solving an operator equation in a Banach space. With the help of the modern notion of functions of bounded variation in multidimension, we prove the convergence of the algorithm.