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51.
The two-step process of hydrogenation of l-alkyl-3-acylpyridinium salts and cyclization of the resultant 1, 4, 5, 6-tetrahydropyridines has been the foundation of a general scheme of alkaloid synthesis.1 Its application in the indole alkaloid field has yielded ready access to tetrahydro-β-carboline systems, e.g. 1a → 2 → eburnamonine.2 Since acid treatment of Nb -acyl derivatives of substances related to la has been shown to lead to products of indole β-cyclization3, it became of interest to test the cyclization behavior of the vinylogous imide lb, prepared by the dicyclohexylcarbodiimide-induced acylation of 3-acetyl-1, 4, 5, 6-tetrahydropyridine4 with indoleacetic acid. Treatment of lb with boron trifluoride gave a 62 yield of ketolactam 3a. Thus a two-step entry into the pentacyclic Aspidosperma alkaloid skeleton is on hand. 相似文献
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Ernest Z. Manson Kyama C. Mutinda Joseph K. Gikunju Aleksandra Bocian Konrad K. Hus Vladimír Petrílla Jaroslav Legth James H. Kimotho 《Molecules (Basel, Switzerland)》2022,27(3)
The administration of toxin-specific therapy in snake envenoming is predicated on improved diagnostic techniques capable of detecting specific venom toxins. Various serological tests have been used in detecting snakebite envenoming. Comparatively, enzyme-linked immunosorbent assay (ELISA) has been shown to offer a wider practical application. We report an inhibition ELISA for detecting three-finger toxin (3FTx) proteins in venoms of African spitting cobras. The optimized assay detected 3FTxs in N. ashei (including other Naja sp.) venoms, spiked samples, and venom-challenged mice samples. In venoms of Naja sp., the assay showed inhibition, implying the detection of 3FTxs, but showed little or no inhibition in non-Naja sp. In mice-spiked samples, one-way ANOVA results showed that the observed inhibition was not statistically significant between spiked samples and negative control (p-value = 0.164). Similarly, the observed differences in inhibition between venom-challenged and negative control samples were not statistically significant (p-value = 0.9109). At an LOD of 0.01 µg/mL, the assay was able to confirm the presence of 3FTxs in the samples. Our results show a proof of concept for the use of an inhibition ELISA model as a tool for detecting 3FTxs in the venoms of African spitting cobra snakes. 相似文献
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Skupinska KA McEachern EJ Skerlj RT Bridger GJ 《The Journal of organic chemistry》2002,67(22):7890-7893
A method to prepare amino-substituted 5,6,7,8-tetrahydroquinolines and 5,6,7,8-tetrahydroisoquinolines via catalytic hydrogenation of the corresponding acetamido-substituted quinolines and isoquinolines followed by acetamide hydrolysis is described. The yields of the products are good when the acetamido substituent is present on the pyridine ring and moderate with the acetamido substituent on the benzene ring. This method has also been applied to the regioselective reduction of quinoline substrates bearing other substituents (R = OMe, CO(2)Me, Ph). 相似文献
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Richard L. Martin Larry E. McMurchie Ernest R. Davidson 《International journal of quantum chemistry》1978,13(2):161-168
The completeness of a basis set for ethylene is examined relative to its ability to describe transition moments. The double zeta (Dunning contraction) plus polarization plus Rydberg Cartesian Gaussian set does much better for length than for velocity moments. An attempt is made to interpret the transition moment sums for the occupied orbitals. 相似文献
60.
The 13C NMR spectra of cyclobutane and seven methylated homologs and of ethyl cyclobutanecarboxylate and five isomeric diethyl cyclobutanedicarboxylates are reported and substituent parameters for methyl groups in methylcyclobutanes are calculated. Of note is a sizeable and nearly configuration-independent upfield shifting γ-effect. 相似文献