Recent advances made in the synthesis of small drug molecules for clinical applications : An insight

Over decades dependency of humans on the drugs has become indispensable and irreplaceable. Thus, each year many new drugs are licensed. Nonetheless, drugs undergo rigorous testing and analysis to be available globally in economic price for the suitability of patients with different age and physiological conditions. The testing of drugs include phase I clinical trial using small group of 20–100 healthy volunteers for safety, pharmacology and efficacy; phase II clinical trial using 100–500 volunteer patients to optimize effective dose, dose interval, safety analysis and mode of delivery such as oral or intravenous; phase III clinical trial using 1000–5000 in a larger population of patients globally at different international places to collect sufficient safety and efficacy data for patenting and licencing. Moreover, thousands of drugs fail to achieve these objectives. Therefore, this mini-review intends to critically examine and assimilate the clinical applications of selected complex repurposed small drug molecules which are in different phase of trials for treating viral infection including complications due to COVID-19: (a) Remdesivir, (b) Galidesivir, (c) Favipiravir, (d) Baricitinib, and (e) Baloxavir

Research Paper Use of cation exchange resins for the synthesis of bis-indolylmethanes

Abstract: Simple and highly efficient procedure for the synthesis of bis-indolylmethanes is described under both solvent and solvent-free conditions with excellent yields. This approach utilizes cation exchange resins as catalyst under mild reaction conditions

Improved One-Pot Synthesis of Citalopram Diol and Its Conversion to Citalopram

An improved process is developed for the preparation of citalopram diol, <b>2</b> which involves two consecutive Grignard reactions in situ followed by an efficient and simple workup process with improved overall yield. Process development efforts for conversion of <b>2</b> into citalopram, <b>1</b>, and a control strategy for impurities are discussed. The present work addresses the challenges associated with the process development and scale-up of citalopram such as handling of unstable intermediates, control of various potential impurities, and process safety to achieve an economic and scalable process

An Efficient Synthesis of 1‑(2-Methoxyphenoxy)-2,3-epoxypropane: Key Intermediate of β‑Adrenoblockers

An efficient process for the preparation of 1-(2-methoxyphenoxy)-2,3-epoxypropane, a key intermediate for the synthesis of ranolazine is described

Improved Process for Preparation of (3<i>R</i>,4<i>R</i>)‑3-(3,4-Dimethyl-4-piperidinyl)phenol, A Key Intermediate for the Synthesis of Alvimopan

This report discloses an industrially feasible and cost efficient process for the preparation of the compound [(3<i>R</i>, 4<i>R</i>)-3-(3,4-dimethyl-4-piperidinyl)­phenol] (<b>1</b>), which is used as the key intermediate for preparation of the opioid drug Alvimopan. The overall yield in this process is increased from 15 to 30%, mainly due to the improvement in yield from 26 to 53% for intermediate <b>7</b>