Please use this identifier to cite or link to this item: 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:Faculty of Chemistry

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01_title.pdfAttached File72.05 kBAdobe PDFView/Open
02_dedication.pdf168.42 kBAdobe PDFView/Open
03_certificates.pdf135.38 kBAdobe PDFView/Open
04_acknowledgements.pdf107.47 kBAdobe PDFView/Open
05_abstract.pdf920.72 kBAdobe PDFView/Open
06_table of contents.pdf108.88 kBAdobe PDFView/Open
07_list of tables and figures.pdf190.89 kBAdobe PDFView/Open
08_list of abbreviations.pdf139.72 kBAdobe PDFView/Open
09_general remarks.pdf162.06 kBAdobe PDFView/Open
10_chapter 1.pdf936.87 kBAdobe PDFView/Open
11_chapter 2.pdf1.92 MBAdobe PDFView/Open
12_chapter 3.pdf3.49 MBAdobe PDFView/Open
13_chapter 4.pdf1.66 MBAdobe PDFView/Open
14_chapter 5.pdf2.64 MBAdobe PDFView/Open
15_chapter 6.pdf903.45 kBAdobe PDFView/Open


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