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Part-1Review on Antiulcer LiteratureNNPyridinepKa : 5.2NPyrimidinepKa : 1.31The weekly basic nature of pyrimidine (pKa 1.31) is striking in relation to pyridine(pKa 5.2). It is understandable as in inductive effect (depletion of π-electrons), caused byinsertion of the avidly electron-attracting second nuclear nitrogen atom. Pyrimidine maytherefore be likened more to beta-nitropyridine (pKa 0.8), which contains the equallystrongly electron-attracting nitro group, than to the parent pyridine. A cursory review ofthe literature does reveal successful use of this logic. Replacement of the pyridine ringwith less basic isosteric pyrimidine ring has also been reported by Japanese workers 81 .They have evaluated2-(1H-benzoimidazole-2-sulfinylmethyl)-4-dimethylaminopyrimidine-5-carboxy-licacid ethyl ester 43 for its proton pump inhibition. It was foundto have marked proton pump inhibitory activity with IC 50 of 7.5 µm as compared toomeprazole IC 50 of 5.8 µm.NONSNONH43NOIt really appears difficult that in this system the formation of the disulfide intermediate islikely. This is owing to the poor availability of electrons on pyrimidine and its nitrogens.38
Part-1Review on Antiulcer LiteratureOONHNSOHNNSOOmerazoleONHONHR 1R 1NNR 2NHNXSNot possibleXOR 2HNNSOPyrimidineNHNHFigure 20: Inability of pyrimidine analog of omeprazole to form sulfenamideintermediate.1.7.5 Some More Literature Reports:Corvi-Mora 106 synthesized derivatives of piperazinyl acetamides 73 possessing anti-ulcerand anti-secretion properties. These compounds were entirely free from anticholinergicactivity. Though mechanism of action is not clear, anti-ulcer activity was evaluatedsuccessfully in different models like reserpine ulcer with rats and phenylbutazonehistamineulcer.NHHNNO73Murai et.al., 107 reported the anti-ulcerative activity of benzoguanamine derivatives 74.39
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Saurashtra UniversityRe - Accredite
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Statement Under O.Ph.D. 7 of Sauras
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ContentsAcknowledgementRegistration
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Contents1.2 Synthesis of condensed
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Contents1.5 MDR modulators 3981.6 D
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infrastructure and all the faciliti
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Above all I thank Lord Hanuman Ji a
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Abbreviations used1 H NMR Proton Nu
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UVVEGFRWCRWHOZ-EUltra VioletVascula
Page 19 and 20: 22. 2-Substitutedthieno[3,2-d]/benz
Page 21 and 22: PrefacePrefaceHeterocyclic chemistr
Page 23 and 24: PrefaceThis entire cascade of react
Page 25 and 26: PrefaceOONHNHPOCl 3MWINVi-xviiClClC
Page 27 and 28: PrefaceOOHOOOONHNHDP-7 1NHMonastrol
Page 29 and 30: PART-I
Page 31 and 32: 3.7 Results and discussion on biolo
Page 33 and 34: Part-1Review on Antiulcer Literatur
Page 37 and 38: Table 2: Distinguishing Features of
Page 41 and 42: 1.2.2. Muscarinic AntagonistsPart-1
Page 55 and 56: 1.5.5. Pharmacological PropertiesPa
Page 69: Part-1Review on Antiulcer Literatur
Page 89 and 90: 2. Aim of the Present WorkPart-IAim
Page 91 and 92: Part-IAim of Present WorkR 2 OR 3 R
Page 93 and 94: 2.2. Bacisity of Pyridine vs Pyrimi
Page 95 and 96: Part-IAim of Present WorkOANNHOSNHN
Page 97 and 98: Part-IAim of Present WorkS. No. A S
Page 99 and 100: 3. Results and Discussion
Page 101 and 102: Part-IResults and Discussion3.1.1d
Page 103 and 104: Part-IResults and DiscussionOR 1XR
Page 105 and 106: Part-IResults and Discussionformed
Page 107 and 108: Part-IResults and DiscussionOOON 2
Page 109 and 110: c. Synthesis of 2-carbethoxy-3-amin
Page 111 and 112: Part-IResults and DiscussionTable 7
Page 113 and 114: Part-IResults and DiscussionOOEtNHO
Page 115 and 116: Part-IResults and DiscussionTable-8
Page 117 and 118: Part-IResults and DiscussionCompd.N
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S. No. Y Mol. Formula(Sol. ofrecrys
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Part-IResults and DiscussionS. No.
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Part-IResults and DiscussionONNHIII
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Part-IResults and DiscussionS. No.A
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Part-IResults and Discussion3.5. Sp
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Specimen 1 H NMR spectra of 2-chlor
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Part-IResults and Discussioninvolve
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Part-IResults and DiscussionSpecime
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The Infrared (IR) spectra:Part-IRes
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Part-IResults and DiscussionR 1ON+
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Part-IResults and DiscussionOSNHOSN
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3.6 Biological Evaluation of PPI’
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Part-IResults and DiscussionExperim
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Part-IResults and DiscussionDrug Pr
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Table 11. Effect of newly synthesiz
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Part-IResults and DiscussionS.No.AR
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Part-IResults and DiscussionS.No.AR
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Figure-1. Effect of newly synthesiz
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Figure-3. Effect of newly synthesiz
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Part-IResults and DiscussionFigure
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Part-IResults and DiscussionFigure
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Part-IResults and Discussion2. Effe
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Part-IResults and Discussionby kine
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Part-IResults and DiscussionNNNNNHN
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3.8. QSAR StudiesPart-IResults and
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Part-IResults and DiscussionFigure-
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Part-IResults and DiscussionPhysico
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Part-IResults and DiscussionThe MDS
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2. Volume of gastric secretion:Desc
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Part-IResults and DiscussionFor the
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Part-IResults and DiscussionTable-1
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3. Ulcer scoreDescription of the de
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Part-IResults and Discussion24. Ros
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4. Experimental
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Part-IExperimental119 o C was 128-1
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5. Synthesis of ethyl 2-amino-4-phe
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Part-IExperimentalthe procedure des
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Part-IExperimentalRecrystallization
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Part-IExperimentalM.P. : 132-134 o
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Part-IExperimentalA solution of thi
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Part-IExperimentalNMR (CDCl 3 )δpp
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Part-IExperimental6. Reaction of et
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Part-IExperimentalNMR (CDCl 3 )δpp
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Part-IExperimentalM.P. : 240-245 o
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Part-IExperimentalrecrystallization
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Part-IExperimental(1H, d, CH at imi
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Part-IExperimentalNMR (DMSO-d 6 )δ
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M.P. : 140-142 o C; Yield: 73%.Mol.
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M.P. : 135-141 o C; Yield: 67%.Mol.
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Part-IExperimentalml), over a perio
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Part-IExperimentalchloride was adde
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Part-IExperimental29. Synthesis of
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Part-IExperimentalIR (KBr) cm -1 :
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Part-IExperimentaladded while stirr
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Part-IExperimentald]pyrimidin-4(3H)
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Part-IExperimentalMol. formula : C
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Part-IExperimentalthis clear soluti
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Part-IExperimentalwhile maintaining
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Part-IExperimentalMol. Formula : C
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PART-II
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Part-IIContents2.3.2.1 Mononuclear
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Part-IISynthesis of Pyrimidines1. S
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Part-IISynthesis of PyrimidinesYZR
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Part-IISynthesis of Pyrimidineselec
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Part-IISynthesis of PyrimidinesR 1R
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Part-IISynthesis of Pyrimidinespyri
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R 1 R 2 R Yield(%)Part-IISynthesis
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Part-IISynthesis of Pyrimidinesyiel
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Table 27: 2-Amino-3-substitutedaryl
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Part-IISynthesis of PyrimidinesWhil
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Part-IISynthesis of PyrimidinesSimi
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Part-IISynthesis of PyrimidinesTabl
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R 1 R 2 R X Yield(%)Part-IISynthesi
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Part-IISynthesis of Pyrimidines+RCN
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Part-IISynthesis of PyrimidinesNN+
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Part-IISynthesis of PyrimidinesR 1+
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Part-IISynthesis of Pyrimidinesthe
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Part-IISynthesis of Pyrimidinesacet
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Part-IISynthesis of Pyrimidinesexpe
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Part-IISynthesis of PyrimidinesNOOC
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Part-IISynthesis of PyrimidinesThe
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Part-IISynthesis of PyrimidinesTabl
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Part-IISynthesis of PyrimidinesOH 3
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1.10 ReferencesPart-IISynthesis of
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Part-IISynthesis of Pyrimidines42.
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2. Impact of Microwave Assisted Hea
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Part-IIImpact of Microwave…Microw
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Part-IIImpact of Microwave…Figure
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Part-IIImpact of Microwave…R 1ArR
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Part-IIImpact of Microwave…as an
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Part-IIImpact of Microwave…al. 21
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Part-IIImpact of Microwave…XOHR 1
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Part-IIImpact of Microwave…N+N21B
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Part-IIImpact of Microwave…OO+ NO
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Part-IIImpact of Microwave…NO 2NO
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Part-IIImpact of Microwave…RNHNNH
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Part-IIImpact of Microwave…assist
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Part-IIImpact of Microwave…CNRNH
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Part-IIImpact of Microwave…Multig
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Part-IIImpact of Microwave…Nie et
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Part-IIImpact of Microwave…synthe
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Part-IIImpact of Microwave…An eff
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Part-IIImpact of Microwave…OO+S 8
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2.6. ReferencesPart-IIImpact of Mic
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49. Baxendale, I. R.; Ley, S. V. J.
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Part-IIAim of the Present Work3. Ai
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Part-IIAim of the Present WorkONHR
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Part-IIAim of the Present WorkYZXNN
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Part-IIAim of the Present WorkThe c
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3.5 References:Part-IIAim of the Pr
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Part-IIAim of the Present Work37. S
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Part-IIResults and Discussion4.1 Sy
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4.2 Synthesis of condensed 2-substi
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Table 38: Physical data of condense
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S. No. X Time ofMWIHeating(Min)VxiV
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S. No. X Time ofMWIHeating(Min)Yiel
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4.3 Synthesis of condensed 4-chloro
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Part-IIResults and DiscussionHerein
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Part-IIResults and DiscussionS. No.
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Part-IIResults and DiscussionS. No.
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The Mass spectraPart-IIResults and
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Specimen IR spectra of some 2-chlor
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Part-IIResults and Discussion1 H NM
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Part-IIResults and Discussionion (c
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Specimen 1 H NMR spectra of 4-chlor
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Part-IIResults and Discussion4.5 MD
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Part-IIResults and DiscussionH 3CO1
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Part-IIResults and DiscussionCl14.
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Part-IIResults and DiscussionO14. V
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4.6 References:Part-IIResults and D
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5. ExperimentalPart-IIExperimentalA
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3. Synthesis of 2-chloromethyl-5-ph
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Part-IIExperimentalIR (KBr) cm -1 :
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Part-IIExperimentalM.P. : 247-249 o
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Part-IIExperimental5.4 Synthesis of
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Part-IIExperimentalwere reacted und
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27. Synthesis of 2-methyl-5-phenylt
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Part-IIExperimental80 o C) that yie
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Part-IIExperimental36. Synthesis of
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Part-IIExperimentalunder microwave
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Part-IIExperimentalM.P. : >300 o C
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M.P. : 280-282 o C; Yield: 90%Mol.
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5.10 References:Part-IIExperimental
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Synthesis, Characterization and Ant
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Part-IIIAdvances Dihydropyridines a
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CH 3CH 3Part-IIIAdvances Dihydropyr
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2. Aim of the Present Work
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Part-IIIAim of the Present Workshor
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3. Results and Discussion
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Part-IIIResults and DiscussionOOOHR
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Part-IIIResults and DiscussionUsing
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Part-IIIResults and DiscussionS. No
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S. No R X MolFormula(Sol. of Recrys
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Part-IIIResults and Discussionpheny
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Specimen 13 C NMR spectra of some D
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Part-IIIResults and DiscussionTable
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Part-IIIResults and DiscussionTable
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3.5 DiscussionPart-IIIResults and D
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4. Experimental
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Part-IIIExperimentalglacial acetic
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Part-IIIExperimental5. Synthesis of
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Part-IIIExperimentalIR(KBr) cm -1 :
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Part-IIIExperimentalM.P. : 184-186
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Part-IIIExperimental1 H NMR(DMSO-d
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Part-IIIExperimentalM.P. : 188-190
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Part-IIIExperimental4.2 MDR reversa
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Summary and Conclusion
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Summary and Conclusionactivity in P
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Summary and Conclusionreverting act
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Publications and Presentations
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Publications and PresentationsOther
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Publications and Presentations8. K.
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