Development of a two-step route to 3-PBC and βCCt, two agents active against alcohol self-administration in rodent and primate models

To gain access to 3-propoxy-β-carboline hydrochloride (3-PBC·HCl) (1·HCl) and β-carboline-3-carboxylate-tert-butyl ester (βCCt) (2), potential clinical agents active against alcohol self-administration, a two-step route was developed. This process involves a palladium-catalyzed Buchwald-Hartwig coupling and an intramolecular Heck reaction. This two-step route provides rapid access to multigram quantities of 3-PBC (1) and βCCt (2), as well as analogues for studies of alcohol self-administration. The overall yield of 3-PBC (1) was improved from 8% to 50% by this route.     

Representations of the optimal filter in the context of nonlinear filtering of random fields with fractional noise

The problem of nonlinear filtering of multiparameter random fields, observed in the presence of a long-range dependent spatial noise, is considered. When the observation noise is modelled by a persistent fractional Wiener sheet, several pathwise representations of the optimal filter are derived. The representations involve series of multiple stochastic integrals of different types and are particularly important since the evolution equations, satisfied by the best mean-square estimate of the signal random field, have a complicated analytical structure and fail to be proper (measure-valued) stochastic partial differential equations. Several of the above optimal filter representations involve a new family of strong martingale transforms associated to the multiparameter fractional Brownian sheet; the latter martingale family is of independent interest in fractional stochastic calculus of multiparameter random fields.     

The Formation of Tetrahydrofuran-Based Hydrate Suspensions in n-Decane as Studied by Near Infrared Spectroscopy

Near infrared spectroscopy and principal component analysis (PCA) have been used for monitoring interactions between THF hydrates and naphthenic acids and other surface active molecules. The hydrate particles are primarily hydrophilic and are preferably localized in the water phase. Interactions with surface active molecules may hydrophobize the hydrate surface sufficiently to disperse them into a paraffinic n-decane phase. Hydrate particles dispersed into the n-decane give rise to light scattering accompanied by a baseline shift in the NIR spectra. These observations serve as proof of such interactions taking place and may in turn contribute to the understanding of natural transportability in pipelines of hydrates in multiphase flow.     

Synthesis of N-substituted indole derivatives via PIFA-mediated intramolecular cyclization

[Structure: see text] A variety of N-arylated and N-alkylated indole derivatives were synthesized by way of a phenyliodine bis(trifluoroacetate) (PIFA)-mediated intramolecular cyclization. This novel method allows for the construction of an indole skeleton by joining the N-atom on the side chain to the benzene ring at the last synthetic step. Other novel pyrrole-fused aromatic compounds can also be achieved by this method.     

THE INFLUENCE OF SODIUM PENTOBARBITAL ANESTHESIA ON in vivo PHOTODYNAMIC THERAPY

Abstract The use of sodium pentobarbital anesthesia 50 jig gm⁻¹ during localized photodynamic therapy (PDT) was examined in C57BL/6 mice transplanted with the pigmented B-16 melanoma. A 10 mg kg⁻¹ i.p. injection of Photofrin II was administered 24 h prior to light exposure (630 nm, 150 mW, cm⁻², 300-500 J cm⁻²). Separate groups of mice were utilized to monitor tumour temperature and PDT tumor response. Core tumor temperatures decreased by approx. 10^oC following sodium pentobarbital administration. Tumor responses were determined by documenting the percentage of treated animals without tumor recurrences for a period of 50 days following PDT. Superior PDT induced tumor responses were obtained in control (non-anesthetized) mice following light doses of 400 and 500 J cm⁻². The results of this study indicate that sodium pentobarbital can induce a protective effect on B-16 melanomas treated with PDT.