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Part-IIImpact of Microwave…BrOB(OH) 2OONHNH+OPd/C, Na 2 CO 3NMP/H 2 O (10:4)MWI, 120 o C,20 minONH51NHOOOBrOOONHONH+OOPd(OAc) 2 P(o-tolyl) 3DIPEA, MeCNMWI, 180 o C,30 minONH52NHOBrHNROONH+H 2 NOPd(OAc) 2 , Xantphos,Cs 2 CO 3 , THFRMWI, 120-150 o C, 15 minOONHONHON OH53R= 3-NHCOCH 3 , 4-NHCOCH 3 etcOBrOONHPd(OAc) 2 [P(o-tolyl) 3 ] 2DIPEA, MeCN, H 2 OMWI, 150 o C,15 minONONHONH54O298
Part-IIImpact of Microwave…Nie et al., 51 reported microwave-assisted reaction of 2’-hydroxychalcones with amidinesor guanidines to synthesize 2,4,6-trisubstitutedpyrimidines 55 (100 compounds).R 2R 1OOH+ArHNR 2 NH 2MWI, 190 o C, 30 minR 1NOH55NArR 1 = H, F, Cl, BrR 2 = Ph, 4-CH 3 Ph, 4-ClPh, cyclopropyl, NH 2An efficient and rapid microwave-assisted solution-phase method for the synthesis of 2-amino-4-arylpyrimidine 5-carboxylic acid derivatives has been developed. The five-steplinear protocol involves an initial Biginelli multicomponent reaction leading todihydropyrimidine-2-thiones 56 which are subsequently S-alkylated with methyl iodide.The resulting 2-methylthiodihydropyrimidines 57 are sequentially oxidized first withmanganese dioxide and then with oxone to provide 2-methylsulfonyl-pyrimidines 58which serve as excellent precursors for the generation of a variety of 2-substitutedpyrimidines 59 via displacement of the reactive sulfonyl group with nitrogen, oxygen,sulfur, and carbon nucleophiles. The use of high-temperature sealed-vessel microwaveirradiation allows the preparation of the desired target structures in high yields andcomparatively short reaction times. 52OPhOPhOPhEtOO+OH 2 NHNH 2TMSClMeCN, DMFEtONHMWI, 120 o C,10 min NHS56MeI, MeCN,MWI, 100 o C, 5 minSNaOH (1M)EtONHNSMeMnO 2 ,MWI, 100 o C20 minOPhOPhOPhEtON59N nucleophile, baseEtOMWI, 70-230 o C, 10 minNuNu= pyrrolidine, piperidine,ethanolamine, amonia, phenol etcN58NOSOxone, H 2 O, MeOHEtOMWI, 100 o C, 20 minON57NSMe299
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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
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22. 2-Substitutedthieno[3,2-d]/benz
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PrefacePrefaceHeterocyclic chemistr
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PrefaceThis entire cascade of react
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PrefaceOONHNHPOCl 3MWINVi-xviiClClC
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PrefaceOOHOOOONHNHDP-7 1NHMonastrol
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PART-I
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3.7 Results and discussion on biolo
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Part-1Review on Antiulcer Literatur
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Table 2: Distinguishing Features of
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1.2.2. Muscarinic AntagonistsPart-1
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1.5.5. Pharmacological PropertiesPa
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2. Aim of the Present WorkPart-IAim
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Part-IAim of Present WorkR 2 OR 3 R
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2.2. Bacisity of Pyridine vs Pyrimi
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Part-IAim of Present WorkOANNHOSNHN
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Part-IAim of Present WorkS. No. A S
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3. Results and Discussion
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Part-IResults and Discussion3.1.1d
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Part-IResults and DiscussionOR 1XR
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Part-IResults and Discussionformed
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Part-IResults and DiscussionOOON 2
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c. Synthesis of 2-carbethoxy-3-amin
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Part-IResults and DiscussionTable 7
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Part-IResults and DiscussionOOEtNHO
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Part-IResults and DiscussionTable-8
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Part-IResults and DiscussionCompd.N
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Part-IResults and DiscussionStep-IY
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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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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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Page 309 and 310: Part-IISynthesis of Pyrimidines42.
Page 311 and 312: 2. Impact of Microwave Assisted Hea
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Page 317 and 318: Part-IIImpact of Microwave…R 1ArR
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Page 347 and 348: 2.6. ReferencesPart-IIImpact of Mic
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Page 363 and 364: Part-IIResults and Discussion4.1 Sy
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Page 375 and 376: Part-IIResults and DiscussionHerein
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Page 381 and 382: The Mass spectraPart-IIResults and
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Part-IIResults and Discussionion (c
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Specimen IR spectra of some 4-chlor
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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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