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buffer consisting of 0.02M Sodium phosphate and 0.01M Octane

sulfonic acid and pH adjusted to 4.2 with dilute phosphoric acid

solution. The analysis is performed on a gradient conditions with

mobile phase A , a mixture of buffer and acetonitrile (90:10,v/v)

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(80:20,v/v). The mobile phase was filtered through a 0.45 µm

nylon membrane and degassed with helium for 5 min. The mobile

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column was maintained at 27 °C and the effluent was monitored at

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SUMMARY AND CONCLUSIONS

STUDIES TOWARDS PROCESS RESEARCH AND DEVELOPMENT OF

FEW BIOLOGICALLY ACTIVE COMPOUNDS CONTAINING

DIHYDROPYRIDINE AND PURINE NITROGEN HETEROCYCLES

Summary

Process research and development entails balancing the aspects of

chemistry, economy, safety, ecology, regulatory, intellectual property

robustness, and quality and yet speed. Coalescing the science,

technology, logic and business organically is the prime responsibility of a

process chemist. To a greater extent this analysis was applied and

demonstrated during the development of Lacidipine, Valacyclovir and

Ganciclovir during the research work.

Conclusions

In conclusion, the research studies presented in this thesis have

contributed to the existing knowledge of scientific community on nitrogen

heterocycles in the following aspects.

1. An improved, cost-viable, and plant-friendly process was developed for

the synthesis of Lacidipine, 1. Thorough understanding of the process

parameters coupled with integrated calorimetric approach ensured

successful design of improved process and well control of all process

related impurities. Investigation on five related substances

emphasizes the quality consciousness during process research.

277

2. The azide chemistry explored for Valacyclovir 49, opens up a new

pathway to prepare other commercially important purine derivatives.

More specifically to circumvent patent barricades so as to offer

affordable medicines to the needy patient population.

3. Explored the usage of chloromethylacetate to eradicate the prevailing

challenges in chloromethylation step and employed masked glycerol

protocol for the synthesis of Ganciclovir, 73. This synthetic strategy

can be extrapolated to other biologically and commercially important

analogues.

4. The frame work demonstrated for addressing GTIs rendered a frame of

reference to the process chemist to offer pharmaceutical products

devoid of GTIs.

Over the years, we at Dr. Reddy‟s with our experienced learning in the

same field, have identified some key areas and we believe that the

research work presented in this thesis would be imperative in the

direction to ensure availability of affordable medicines with highest

quality in the most economical, robust, safe, rapid, and environment

friendly way to the patient population.