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http://hdl.handle.net/10603/4519
Title: | Synthesis and characterization of some active pharmaceutical Indole derivatives and their analogs |
Researcher: | Gilla, Goverdhan |
Guide(s): | Reddy, Ghanta Mahesh Himabindu, V |
Keywords: | Active Pharmaceutical Ingredients Zafirlukast Chemistry |
Upload Date: | 3-Sep-2012 |
University: | Jawaharlal Nehru Technological University |
Completed Date: | May, 2011 |
Abstract: | Thesis entitled ?SYNTHESIS AND CHARACTERIZATION OF SOME ACTIVE PHARMACEUTICAL INDOLE DERIVATIVES AND THEIR ANALOGS? has been presented as five chapters.Chapter-1 deals with the general introduction and biological importance of indole derivatives and fused indole derivatives. Also presents, a brief introduction to process development, importance of impurity profile (Related substances) and polymorphic studies in the process development. Chapter-2 comprises process development of zafirlukast, an anti-asthma drug, preparation of stable amorphous and new acetonitrile solvate polymorph. Chapter-3 deals with a complete impurity profile of zafirlukast including identification, synthesis, characterization and root cause of their formation. Chapter-4 explains the synthesis and characterization of new zafirlukast related analogs. Chapter-5 presents an alternative synthesis of tadalafil from D-tryptophan and sarcosine ethyl ester. Described the impurity profile of two commercial viable schemes with the identification, synthesis, characterization and root cause of their formation.Chapter-1: Introduction to process development of APIs and a brief review on indole and fused indole derivatives In this chapter introduction and biological importance of indole derivatives and fused indole derivatives were described. Also, a brief introduction to the process development, importance of impurity profile and polymorphic studies in the process development was presented.Chapter-2: An improved process for the preparation of Zafirlukast-an anti asthma drug Zafirlukast (1) is a selective and competitive oral leukotriene receptor antagonist (LTRA) marketed under the brand name accolate.Figure 1: Zafirlukast 1 Explains the improved synthesis for zafirlukast from 3-methoxy-4-methyl benzoicacid 2 (scheme 1). Esterification of acid 2 in the presence of thionyl chloride in methanol produced ester 3, which was subjected to benzylic bromination under DBDMH and AIBN in cyclohexane to provide bromo derivative. |
Pagination: | 230p. |
URI: | http://hdl.handle.net/10603/4519 |
Appears in Departments: | Department of Chemistry |
Files in This Item:
File | Description | Size | Format | |
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01_title.pdf | Attached File | 72.05 kB | Adobe PDF | View/Open |
02_dedication.pdf | 168.42 kB | Adobe PDF | View/Open | |
03_certificates.pdf | 135.38 kB | Adobe PDF | View/Open | |
04_acknowledgements.pdf | 107.47 kB | Adobe PDF | View/Open | |
05_abstract.pdf | 920.72 kB | Adobe PDF | View/Open | |
06_table of contents.pdf | 108.88 kB | Adobe PDF | View/Open | |
07_list of tables and figures.pdf | 190.89 kB | Adobe PDF | View/Open | |
08_list of abbreviations.pdf | 139.72 kB | Adobe PDF | View/Open | |
09_general remarks.pdf | 162.06 kB | Adobe PDF | View/Open | |
10_chapter 1.pdf | 936.87 kB | Adobe PDF | View/Open | |
11_chapter 2.pdf | 1.92 MB | Adobe PDF | View/Open | |
12_chapter 3.pdf | 3.49 MB | Adobe PDF | View/Open | |
13_chapter 4.pdf | 1.66 MB | Adobe PDF | View/Open | |
14_chapter 5.pdf | 2.64 MB | Adobe PDF | View/Open | |
15_chapter 6.pdf | 903.45 kB | Adobe PDF | View/Open |
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