Showing papers on "Thiazepine published in 2020"

Direct Amine-Catalyzed Enantioselective Synthesis of Pentacyclic Dibenzo[b,f][1,4]oxazepine/Thiazepine-Fused Isoquinuclidines along with DFT Calculations.

Abstract: A direct protocol for the asymmetric synthesis of dibenzoxazepine/thiazepine-fused [2.2.2] isoquinuclidines is developed. The reaction proceeds through a proline-catalyzed direct Mannich reaction followed by an intramolecular aza-Michael cascade sequence between 2-cyclohexene-1-one and various tricyclic imines, like dibenzoxazepines/thiazepines, as an overall [4 + 2] aza-Diels-Alder reaction. A series of pentacyclic isoquinuclidines have been prepared, with complete endo-selectivity, in good to high yields and excellent enantioselectivity (>99:1). Density functional theory (DFT) calculations further support the observed high stereochemical outcome of the reaction.

Synthesis of Azoloquinazolines and Substituted Benzothiazepine as Antimicrobial Agents

Abstract: Background & objective Quinazolines and their fused systems are noteworthy in pharmaceutical chemistry due to their wide range of biological activities. Methods A direct and efficient approach for the synthesis of new series of fused quinazolines with triazole, thiazole, benzimidazole and tetrazole has been preceded via the reaction of quinazoline thione derivative with halogenated compounds or cyclocondensation of arylidene of quinazoline derivative with heterocyclic amines. Also, dibenzo[b,e][1,4]thiazepine derivatives was synthesized through the reaction of 2,6-bis-(2-chloro-benzylidene)-cyclohexanone with o-aminothiophenol. Results The structures of all new synthesized heterocyclic compounds were confirmed and discussed on the bases of spectral data. The utility of the preparation and design of the above mentioned compounds has been shown to be clear in the results of their antimicrobial activity which revealed that some derivatives have potent activity exceeding or similar to the activity of the reference drugs. Conclusion The insertion of triazole or thiazole moieties to be fused with quinazoline ring helps to enhance its antimicrobial activity.

Some Features of the Reactions of 3-Nitro-6-phenylhexa-3,5-dien-2-one with Thiophenols

Abstract: The reaction of 3-nitro-6-phenylhexa-3,5-diene-2-one with 4-methyl- and 4-chlorothiophenols yields 1,4- and 1,6-addition products at conjugated dienone system By the example of the 1,4-addition adduct of 4-methylthiophenol, its conversion in solution to the 1,6-addition product was shown 4-Methyl-3-nitro-2-styryl-2,3-dihydrobenzo[b][1,4]thiazepine was synthesized by reacting 3-nitro-6-phenylhexa-3,5-dien-2-one with o-aminothiophenol

311--6--611-[cf][12] 55- A process for preparing 311-Dichloro-6-methyl -611-dihydrodibenzo[cf][12]thiazepine 55-dioxide

Abstract: The present invention relates to a method for preparing 3,11-dichloro-6-methyl-6,11-dihydrodibenzo[c,f][1,2]thiazepine 5,5-dioxide. More particularly, the present invention relates to a method for preparing high-purity 3,11-dichloro-6-methyl-6,11-dihydrodibenzo[c,f][1,2]thiazepine 5,5-dioxide at a high yield under safe atmosphere through a quantitative reaction without introduction of an excessive amount of hydrogen chloride gas from the outside by substituting the hydroxyl group of 3-chloro-6-methyl-6,11-dihydrodibenzo[c,f][1,2]thiazepine-11-ol 5,5-dioxide as a starting material with a chloride group by means of hydrogen chloride gas generated in situ under the environment of acetyl chloride and the same equivalent of alcohol.

Synthesis of Diverse Fused Tetracyclic Thiazepine-Chalcone Derivatives byClaisen-Schmidt Condensation Reaction and their Antimicrobial Activity

Abstract: To develop antimicrobial agent, a series of thiazepine-chalcones was synthesized by Claisen-Schmidt condensation between the couplings of aryl ketone in three steps protocol and different aromatic aldehydes under strong base catalyst at room temperature. The characterization of final products were carried out by IR, 1H & 13C NMR and elemental analysis. The synthesized compounds were also evaluated for their antibacterial and antifungal activities using specific Gram positive and Gram-negative bacterial strains using cup plate method.