An efficient stereoselective synthesis of aminocyclohexenes from 7-azanorbornenes via LiAlH4 mediated tandem double bond migration-ring opening sequence

hNav1.7 had received great interest in the past decade owing to its attractive mechanism of actions in pain processing pathway. More recently, we developed a series of efficacious hNav1.7 inhibitors for analgesic, which were characterized with a novel aminocyclohexene as pharmacophore. Herein, we reported our synthetic efforts to construct the unique scaffold, which can be rapidly accessed from readily available 7-azanorbornenes via an unexpected catalyst-free, LiAlH₄ mediated tandem double bond migration-ring opening sequence. A probable mechanism was proposed to illuminate the good regio- and stereoselectivity.     

On normal approximation of discounted and strongly mixing random variables

We estimate the difference for bounded functions h: ℝ → ℝ satisfying the Lipschitz condition, where Z _v = B _v ⁻¹ ∑ _i=0 ^∞ v ⁱ X _i and with discount factor ν such that 0 < ν < 1. Here {X _n , n ≥ 0} is a sequence of strongly mixing random variables with , and N is a standard normal random variable. In a particular case, the obtained upper bounds are of order O((1 − ν)^1/2). Published in Lietuvos Matematikos Rinkinys, Vol. 47, No. 3, pp. 399–409, July–September, 2007. The research was partially supported by the Lithuanian State Science and Studies Foundation, grant No. T-15/07.     

An unconstrained optimization method using nonmonotone second order Goldstein's line search

In this paper,an unconstrained optimization method using the nonmonotone second order Goldstein's line search is proposed.By using the negative curvature information from the Hessian, the sequence generated is shown to converge to a stationary point with the second order optimality conditions.Numerical tests on a set of standard test problems confirm the efficiency of our new method.     

Global existence theory and chaos control of fractional differential equations

In this paper, the initial value problem for a class of fractional differential equations is discussed, which generalizes the existent result to a wide class of fractional differential equations. Also the theoretical result established in the paper ensures the validity of chaos control of fractional differential equations. In particular, feed-back control of chaotic fractional differential equation is theoretically investigated and the fractional Lorenz system as a numerical example is further provided to verify the analytical result.     

Linking-Preserving Perturbations of Symmetric Functionals

We consider paths of functionals starting with one which is invariant under the action of an arbitrary group of symmetries. We give conditions for the existence of an unbounded sequence of critical values of the non-symmetric functional at the end of the path in terms of the growth of the critical values of the symmetric one. We apply this to obtain a multiplicity result for a system of elliptic equations whose symmetries are perturbed by a linear term and a non-homogeneous boundary condition.     

Numerical solution of Burgers’ equation by the Sobolev gradient method

Burgers’ equation is solved numerically with Sobolev gradient methods. A comparison is shown with other numerical schemes presented in this journal, such as modified Adomian method (MAM) [1] and by a variational method (VM) which is based on the method of discretization in time [2]. It is shown that the Sobolev gradient methods are highly efficient while at the same time retaining the simplicity of steepest descent algorithms.     

Presmoothing the transition probabilities in the illness-death model

One major goal in clinical applications of multi-state models is the estimation of transition probabilities. In a recent paper, Meira-Machado et al. (2006) introduce a substitute for the Aalen-Johansen estimator in the case of a non-Markov illness-death model. The idea behind their estimator is to weight the data by the Kaplan-Meier weights pertaining to the distribution of the total survival time of the process. In this paper we propose a modification of Meira-Machado et al. (2006) estimator based on presmoothing. Consistency is established. We investigate the finite sample performance of the new estimator through simulations. Data from a study on colon cancer are used for illustration purposes.     

On the convergence rate and some applications of regularized ranking algorithms

This paper studies the ranking problem in the context of the regularization theory that allows a simultaneous analysis of a wide class of ranking algorithms. Some of them were previously studied separately. For such ones, our analysis gives a better convergence rate compared to the reported in the literature. We also supplement our theoretical results with numerical illustrations and discuss the application of ranking to the problem of estimating the risk from errors in blood glucose measurements of diabetic patients.     

奇异摄动初值问题的一致收敛有限差分法

通过一阶和二阶导数讨论了带小参数的线性二阶常微分方程的初值问题.在均匀网格上得出了带常数拟合因子的指数型拟合差分格式,给出了离散最大模意义上的一阶一致收敛性.文中给出了数值结果.