An improved synthesis of isonitrosoacetanilides

A novel two-step synthesis of isonitrosoacetanilides [2-(hydroxyimino)-N-phenylacetamides] has been developed, involving the initial acylation of aniline derivatives with 2,2-diacetoxyacetyl chloride, followed by reaction with hydroxylamine hydrochloride. The method works equally well with a variety of different aniline derivatives, including those with poor aqueous solubility and those containing electron rich ortho-substituents, neither of which react well under traditional conditions.     

Benzothiazolium derivatives. III. Nucleophilic substitution reactions of benzothiazolium salts

The reactions of 2,3-dihydrothiazolo[2,3-b]benzothiazolium bromide 1 (A^? ?Br^?) with certain nucleophilic reagents have been performed for the purpose of ascertaining the reaction pathways and identifying the group that is displaced from the central carbon atom of the dithiocarbamate system. The nature of complex salt-like intermediates formed initially from 1 (A^? ?Br^?) has been studied and confirmed. For comparison, a number of nucleophilic substitution reactions of 2-methylthio-3-methylbenzothiazolium iodide 17 and 2-dimethylamino-3-methylbenzothiazolium perchlorate 18 have been examined.     

A new short synthesis of 3-substituted 5-amino-1-(chloromethyl)-1,2-dihydro-3H-benzo[e]indoles (amino-CBIs)

A new short synthesis of 3-substituted 5-amino-1-(chloromethyl)-1,2-dihydro-3H-benzo[e]indoles from Martius Yellow is disclosed. The key steps of the synthesis were three efficient regioselective reactions (iodination, 5-exo-trig aryl radical-alkene cyclization and carboxylation).     

An Efficient Large Scale Synthesis of 2-Methoxytetrahydrophenanthridine.

A practical and high yielding synthesis of 2-methoxy-7,8,9,10-tetrahydrophenanthridine suitable for large-scale preparation is described.     

Cyclosporin Measurement – who cares about inaccuracy?

Most medical laboratories measure the immunosuppressive drug cyclosporin using one of a number of commercial immunoassays, or high-performance liquid chromatography (HPLC). The calibration of these assays is based on material supplied by the kit manufacturers or prepared in-house. We have examined inaccuracy for the measurement of cyclosporin in samples spiked to known concentrations and the impact of any inaccuracy on the results for cyclosporin measurement in pooled samples from patients prescribed the drug. The data were from the International Cyclosporin Proficiency Testing Scheme, based on aliquots of cyclosporin-free blood to which known amounts of the drug had been added or aliquots of pooled samples collected from patients receiving cyclosporin. Compared with the results using HPLC, the immunoassays had a median bias which ranged from –4.5% to 8.2% for the spiked samples. When pooled samples from patients were analysed the percentage difference from the measured HPLC value, allowing for assay inaccuracy, was as high as 29.9%. It is concluded that inaccuracy is a factor in between-assay performance for this measurement and that proficiency testing schemes should attempt to put more emphasis on this aspect of assay performance.     

The identification problem for complex-valued Ornstein–Uhlenbeck operators in $$L^p(\mathbb {R}^d,\mathbb {C}^N)$$

In this paper we study perturbed Ornstein–Uhlenbeck operators

$$\begin{aligned} \left[ \mathcal {L}_{\infty } v\right] (x)=A\triangle v(x) + \left\langle Sx,\nabla v(x)\right\rangle -B v(x),\,x\in \mathbb {R}^d,\,d\geqslant 2, \end{aligned}$$

for simultaneously diagonalizable matrices \(A,B\in \mathbb {C}^{N,N}\). The unbounded drift term is defined by a skew-symmetric matrix \(S\in \mathbb {R}^{d,d}\). Differential operators of this form appear when investigating rotating waves in time-dependent reaction diffusion systems. We prove under certain conditions that the maximal domain \(\mathcal {D}(A_p)\) of the generator \(A_p\) belonging to the Ornstein–Uhlenbeck semigroup coincides with the domain of \(\mathcal {L}_{\infty }\) in \(L^p(\mathbb {R}^d,\mathbb {C}^N)\) given by

$$\begin{aligned} \mathcal {D}^p_{\mathrm {loc}}(\mathcal {L}_0)=\left\{ v\in W^{2,p}_{\mathrm {loc}}\cap L^p\mid A\triangle v + \left\langle S\cdot ,\nabla v\right\rangle \in L^p\right\} ,\,1<p<\infty . \end{aligned}$$

One key assumption is a new \(L^p\)-dissipativity condition

$$\begin{aligned} |z|^2\mathrm {Re}\,\left\langle w,Aw\right\rangle + (p-2)\mathrm {Re}\,\left\langle w,z\right\rangle \mathrm {Re}\,\left\langle z,Aw\right\rangle \geqslant \gamma _A |z|^2|w|^2\;\forall \,z,w\in \mathbb {C}^N \end{aligned}$$

for some \(\gamma _A>0\). The proof utilizes the following ingredients. First we show the closedness of \(\mathcal {L}_{\infty }\) in \(L^p\) and derive \(L^p\)-resolvent estimates for \(\mathcal {L}_{\infty }\). Then we prove that the Schwartz space is a core of \(A_p\) and apply an \(L^p\)-solvability result of the resolvent equation for \(A_p\). In addition, we derive \(W^{1,p}\)-resolvent estimates. Our results may be considered as extensions of earlier works by Metafune, Pallara and Vespri to the vector-valued complex case.