2-(Bromomethyl)-1-sulfonylaziridines were converted into novel 3-sulfonamido-2,3,4,5-tetrahydro-1,5-benzothiazepines upon treatment with 2-aminothiophenol in THF in the presence of K2CO3. Starting from 3-substituted 2-(sulfonyloxymethyl)aziridines, a regio- and stereocontrolled synthesis of trans-2-phenyl- and trans-4-(phenyl or propyl)-3-sulfonamido-2,3,4,5-tetrahydro-1,5-benzothiazepines was ...

Maca, a plant native to the Peruvian highlands, contains (1R,3S)-1-methyl-1,2,3,4-tetrahydro-beta-carboline-3-carboxylic acid (MTCA). The family of the tetrahydro-beta-carbolines has been associated with both biologically helpful and harmful compounds. We present evidence that MTCA is a natural constituent of Maca, and on consumption no toxicity is found. This suggests that, when consumed as mu...

The NCNN group is an essential part of various heterocycles bearing high biological activities. 1,2,4-Triazines and their condensed derivatives found applications as pharmaceuticals and in agriculture. For example vardenafil ñ phosphodiesterase inhibitor, is useful in the treatment of male erectile dysfunctions (1), apazone exhibit anti-inflammatory and analgesic actions (2), lamotrigine is use...

Based on the dramatic accelerating effect of 2-aminophenol, three ligands derived from 2-aminophenol were developed. Copper-catalyzed coupling reaction of nitrogen-containing nucleophiles with aryl bromides was efficiently carried out under mild conditions using 1,2,3,4-tetrahydro-8-hydroxyquinoline as a novel, simple, and versatile ligand.

Microwave assisted new aldol condensation reaction of 1-oxo-1,2,3,4tetrahydrocarbazoles 1 with thiophene-2-carbaldehyde 2 in the presence of alcoholic KOH affords a single product 2-Thiophen-2-ylmethylene-2,3,4,9-tetrahydro-carbazol-1-one 3. 3 on irradiation with hydroxylamine hydrochloride yielded 3-Thiophen-2-yl-4,5-dihydro-10H-2-oxa-1,10-diazacyclopenta[a]carbazole 4 and 3 on irradiation wit...

An unknown impurity in the fermentation-based drug substance lovastatin at 0.52 RRT was observed invariably in all batches when analyzed by HPLC as per the PhEur monograph. This impurity was isolated from the impurity-enriched sample using reversed-phase preparative HPLC and characterized by using spectroscopic (PMR, CMR, MASS, and UV) techniques as the structurally-related compound Monacolin-X...

The carcinogenicity of 1,11-dimethylchrysene (=5,7dimethylchrysene) and its 1,2,3,4-tetrahydro-, 3,4-dihydro-, and 1,2,3,4-tetrahydro-l-oxo derivatives was tested by mouse skin painting. Each mouse received 30 ¿/gof the chrysene on the dorsal skin twice weekly for one year, and the animals were observed for a second year. The 1-ketone was much more active than any of the hydrocarbons. Of the l...