Synthesis process development of Potential Biologically active new compounds as drug intermediates

Abstract

The present research aims of simplifying the present methodologies of drug synthesis to achieve newlinethe desired products with better yields and high purity. For this purpose the reported synthetic newlineroutes for various important drug ingredients are investigated. The hitherto unknown side newlineproducts / impurities in the different methods are characterized. The studies on the synthesis of newlinedifferent active pharmaceutical ingredients, such as anti-inflammatory drug, Balsalazide, anticonvulsant newlinedrug, Pregabalin, anti-diabetic drug, Sitagliptin, anti-hypertensive drug, Bisoprolol, newlineanti-cholinergic drug, Glycopyrrolate and anti-depressant drug, Escitalopram are described as newlinechapter - I to chapter - VI respectively. newlineCHAPTER I: Studies on the synthesis of anti-inflammatory drug, Balsalazide newlineBalsalazide disodium represents an effective gastrointestinal anti-inflammatory compound newlineuseful as a medicament for the treatment of diseases such as ulcerative colitis. Present work newlineuncovered a new synthetic process to prepare Balsalazide disodium consisting no isolation of newlineany intermediate followed by identification/ preparation/ characterization of related substances, newlinedifferent analogs and positional isomers. newlineApproach A: Balsalazide, consisting three steps, was prepared from 4-nitrobenzoic acid newlinewithout isolation of any intermediate using water as a solvent Scheme-1. newlineDuring process development, eight impurities namely Des-and#946;-alanine Balsalazide, Balsalazide and#946;- newlinealanine, Balsalazide 3-isomer, Decarboxy Balsalazide, Bis-azo salicylic acid, Biphenyl-azo newlinesalicylic acid, Bis-azo diacid and Bis-azo triacid were observed. Present work describes the newlinesynthesis and characterization of these impurities. newline