Microwave Assisted Facile Synthesis and Biological Evaluation of Novel 2-Indolyl -1, 5-Benzothiazepines

Abstract

Abstract:Background:

Synthesis of the 1,5‐Benzothiazepane Scaffold – Established Methods and New Developments

“…As the catalyst was water‐soluble, it could easily be removed and product 62 was purified by recrystallization from ethanol (Figure 18 ). [66] …”

“…As the catalyst was water-soluble, it could easily be removed and product 62 was purified by recrystallization from ethanol (Figure 18). [66] In the next example, the benefits of microwave irradiation and the solvent polyethylene glycol (PEG-400) have been combined. This green solvent is inexpensive, non-halogenated, degradable and shows low toxicity, making it an excellent candidate as a substitute for volatile organic solvents in sustainable chemistry approaches.…”

Chalcone derived benzoheterodiazepines for medicinal applications: A Two‐pot and one‐pot synthetic approach

“…The yield from microwave was higher (82%-95%) than the conventional reflux (55%-74%) with a shorter reaction time [150]. Another heterocyclic molecule of indol-benzothiazepines (35) has also been prepared from chalcone condensation using microwave irradiation with zirconyl chloride as a catalyst [151] (Scheme 9). Both heterocyclic benzodiazepines are pharmacologically active with good to excellent antiinflammatory, antimicrobial, and anticonvulsant activities.…”

“…The bromo substituent in compound (34) gave highly potent antimicrobial action due to the lipophilicity of bromo substituent, which plays a vital role to enhance the lipophilicity of compounds and inhibit microbial infections [150]. Compound (35) showed better anticonvulsant activity and CNS depressant activity than the control with the involvement of sulfur moiety in benzothiazepine and indole [151].…”