Simple thiazocine-2-acetic acid derivatives via ring-closing metathesis

A new protocol for synthesis of 2-heterocylylacetic acid derivatives involving conjugate addition of allyl mercaptan to an acrylate containing a tethered olefinic site followed by RCM (ring-closing metathesis) is described. In this series, sulfanyl derivatives were unreactive, while sulfoxide and sulfone analogues provided the corresponding thiazocines in fair to excellent yields. Use of the sulfoxide oxidation state as a protecting group for sulfides inert to RCM is demonstrated also. Thus, oxidation of sulfide 9 [N-allyl-N-[2-(allylthio)-4-(1H-indol-1-yl)-4-oxobutyl]-4-methylbenzenesulfonamide] followed by cyclization yielded the corresponding thiazocine sulfoxide 12. Deprotection (deoxygenation) of 12 was accomplished using Lawesson's reagent, producing 1-[[4-[4-(methylphenyl)sulfonyl]-3,4,5,8-tetrahydro-2H-1,4-thiazocin-2-yl]acetyl]-1H-indole (21) in 67% unoptimized yield.     

煤中有机硫形态结构和热解过程硫变迁特性的研究

利用热解 质谱并结合固定床热解反应装置，对煤中有机硫的形态主其对加氢热解过程 变迁特性的影响，进行了较系统的研究。结果表明，煤中有机硫的形态结构在褐煤中主要以脂肪族、芳香族硫化物为主，而在 煤中则主要以各种不同芳构化程度的噻吩结构为主，初步表明煤中有机硫形态结构随煤变质程度的变迁呈较强的连续递变性。煤热解过程中硫在呼产物中的变迁和分布与煤中有机硫的形态结构特点密切相关。较高芳构化噻吩结构不完全的氧     

LC–MS Determination and Pharmacokinetic Study of a Novel Sulfonylurea: Potential Hypoglycemic Agent in Rat Plasma

To support preclinical pharmacokinetic investigation of 1-[4-[2-(4-bromobenzene-sulfonaminoethyl)phenylsufonyl]-3-(trans-4-methylcyclohexyl)urea (G004), a rapid, sensitive and specific high-performance liquid chromatography–electrospray ionization mass spectrometry (LC–ESI-MS) method was developed and validated. Glibenclamide was employed as internal standard. After liquid–liquid extraction the analyte was analyzed on a Kromasil C₁₈ column (150 × 2.0 mm i.d.) with a mobile phase consisted of acetonitrile–water (0.05% acetic acid), 30:70 (v/v). The flow rate was 0.2 mL min⁻¹. Detection was performed on a quadrupole mass spectrometer using an electrospray ionization interface and the selected-ion monitoring (SIM) mode. The retention time was about 3.5 and 4.2 min for Glibenclamide and G004, respectively. The assay was linear over the concentration range of 2.0–500.0 ng mL⁻¹. Extraction Recovery of G004 in rat plasma was more than 87%. The intra- and inter-assay precision was lower than 11.5% (CV). This validated method was successfully applied to the pharmacokinetics of G004 in rats.     

Divergence Criterion for a Class of Random Series Related to the Partial Sums of I.I.D. Random Variables

Journal of Theoretical Probability - Let $$ \{X, X_{n};~n \ge 1 \}$$ be a sequence of independent and identically distributed Banach space valued random variables. This paper is devoted to...     

Outcome regression-based estimation of conditional average treatment effect

Annals of the Institute of Statistical Mathematics - The research is about a systematic investigation on the following issues. First, we construct different outcome regression-based estimators for...     

The finite steps of convergence of the fast thresholding algorithms with f-feedbacks in compressed sensing

Numerical Algorithms - Iterative algorithms based on thresholding, feedback, and null space tuning (NST+HT+FB) for sparse signal recovery are exceedingly effective and efficient, particularly for...     

Fast projection onto the ordered weighted ℓ1 norm ball

In this paper,we provide a finitely terminated yet efficient approach to compute the Euclidean projection onto the ordered weighted?₁(OWL1)norm ball.In particular,an efficient semismooth Newton method is proposed for solving the dual of a reformulation of the original projection problem.Global and local quadratic convergence results,as well as the finite termination property,of the algorithm are proved.Numerical comparisons with the two best-known methods demonstrate the efficiency of our method.In addition,we derive the generalized Jacobian of the studied projector which,we believe,is crucial for the future designing of fast second-order nonsmooth methods for solving general OWL1 norm constrained problems.     

Semicontinuity of multiple integrals onW k,p (Ω, ℜ m )(k≥1)

This paper shows thatW ^1,p -quasiconvexity is a necessary and sufficient condition of swlsc (sw*lsc) for multiple integrals with a Caratheodory function as the variational function, bounded by