P.G. Di pl oma - Pharm ac eutic al Chemi stry Paper 1 Organic Chemistry

UNI T 1: Reacti on Mec hanism

Re act i ve i nt er me di ates - Car boca ti ons, Car ba ni ons, Fre e ra dic al s, Car benes a nd nitr enes – Gui del ines f or pr opos ing r ea sonabl e me c ha nis m - I nte r me diat es - K ineti c a nd Ther modyna mi c c ontr ol – me t hods of de ter mi ni ng re ac tion me c ha nis m.

UNI T 2 : St ere oc hemi str y

Ele me nts of s ymme t r y, Chir alit y, M ol ec ule s wit h more t ha n one chir al ce ntr e Re solut ion - Me thods of re sol uti on – Ster os pecif ic a nd Ste re os ele cti ve s ynthes is -Ra ce mi sat ion.

UNI T 3 : Reage nt s i n organic s ynt he sis

O xi dat ion: Oxi dati ons us ing M nO 2 , Se O 2 , Pb( OAC) 4 , Os O 4 , Perac ids, PCC a nd PDC

Re duc tion: Re ducti on usi ng Li AIH 4 , NaBH 4 , W il kinson&a pos ;s c atal ys t, Li ndl ar c ata l yst, BH s / T HF and 9-BBN.

UNI T 4: Ret ro s ynt he si s

Synt hone s - Synt het ic Equi val ent - Tar ge t M ol ec ule - Functi onal Gr oup Inte r c onvers ion. Guideli nes t o a Good Di sc onnec tion – 1,2 - 1,3 - 1,4 -1,5 a nd 1,6 Di f uncti onal Dis conne cti ons .

UNI T 5: Nat ur al pr oduct s chemi str y

Car bohydrate s : Cla ss ific ati on – St ructura l eluci dat ion of gl ucose a nd f ructose – Di sa cc hari de s. St ruct ura l el uci dat ion of sucrose , ma l t ose a nd l act os e– Che mi str y of s tar ch and cel lul os e .

Ste roids : Clas sif ica tion – Study of Vit a mi n D, Estr one , Pr ogest rone, Te stost erone and Androst er one.


Al kaloids : Clas sif ica tion – Ge ne ral Study of Papa veri ne , Morphi ne , and Quinine.

Ref e re nc es : 1. Adva nce d Or ga nic Che mi st r y, Reac tion Mec ha ni s m a nd Str uc tur e, J err y M arc h, J ohn W ile y & s ons 4 t h Edn. 1992. 2. A Guide book t o Me chanis m i n Or ga nic Che mi str y, Pe ter Skye s , Longma n. 3. Ste re o Che mi st r y of Or ga nic Compounds , Ernest L Eliel , Sa muel H.wile n, J ohn Wile y & Sons , Inc . 2003. 4. Ste re o Che mis tr y of Or ga ni c Compounds, D.Na sipuri , Wile y Ea ste rn Lt d., 1991. 5. Pri nci pl es of Or ga ni c Synt he sis , Nor ma n a nd J .M .Coxa n, ELBS 3 r d Edn. 1993. 6. Guide book t o Or ga ni c Synthesi s , R.M .M ac ki e a nd D.M .Smi t h, ELBS, 1982. 7. Or ga ni c Synt he sis , Mic ha el B.Smi th, M.C.Gr a w Hi ll , l nt ernati onal Edn. 1994. 8. M ode m Syntheti c Rea cti ons , H.O.House , Ca mbri dge Uni ve rsi t y Pre ss , 3 r d Edn. 1972 9. Some M odern Met hod of Or ga ni c Synthesi s, W .Ca ruthers , Ca mbri dge Uni vers it y 1972. 10. Or ga ni c Synthes is Conce pt s, Me thods a nd Sta rti ng Mat eri als , Fur thr hop Pe nzl in Ve rla g Che mi e , 1983. 11. Or ga ni c Synt he sis , the di sc onne cti on a ppr oa ch, St ua rt War re n, J ohn Wi le y & Sons . 1992. 12. Or ga ni c Che mi str y, I.L.Fi na r, V ol.ll , ELBS, 5 t h Edn.1975. Paper 2 Analytical Techniques Unit 1: Chromatographic Techniques Principle - Classification of Chromatography - Paper Chromatography TLC-Column chromatography - Ion Exchange Chromatography - Gas Chromatography and HPLC. Unit 2: Spectrophotometric methods of analysis Laws of absorption - Lambert's and Beer's law - Principle and applications of Photometry, Fluorimetry and Flame spectrophotometry. Unit 3: Volumetric methods of analysis Acid - Base titrations - Complexometric titrations - EDTA titrations and metal ion indicator. Unit 4: UV, IR,and NMR Techniques UV-Visible Spectroscopy : Principle - Instrumentation - Electronic Excitation -Applications.


IR Spectroscopy : Principle -Mode of vibrations of a molecule - Instrumentation - Identification of the sample - Characteristic group frequencies. NMR Spectroscopy : Principle - Chemical shift - Peak area - Instrumentation -Spin-spin splitting - Spin relaxation - Shift reagents - Deutrium Substitution-Applications. Unit 5: Industrial effluent treatment Classification of effluents - Treatment of mineral effluents by Ion-exchange, Reverse osmosis and Reagents methods - Treatment of organic effluents by biological oxidation, chlorination and adsorption. References : 1. Instrumental Methods of Analysis H.H. Willard, L.L.Merritt,J.A.Dean,F.A.Settle, CBS Publishers & Distributors, 1986. 2. Instrumental methods of chemical analysis, Gurdeep R.Chatwal,Sham K.Anand,5th Edn., 2003. 3. Principles and practice of analytical chemistry, F. W. Fifield and D.kealey,5th Edn., 2000. 4. Fundamental of analytical chemistry, D.A.Skoog and D.M.,West,Saunders college publishing Cp., Philadelphia, 1982. 5. William Kemp,Organic Spectrocopy, ELBS, 3rd Edn.,1991. 6. R.M.Silverstine, G.C.Bassler, J.C.morril, Spectroscoipc identification of organic compounds,john wiley & sons INC 5th Edn.,1991 7. Industrial Chemistry, B.K.Sharma, Goel publishing House, Edn.XIV,2004

Paper 3 Fundamentals of Pharmaceutical Chemistry

Unit 1: B as ic c once pts

De finiti on of drug – Cl ass ifi cati on of dr ug ba se d upon mode of a cti on and c he mi c al nat ur e - De f ini tion of Phar ma c oki neti cs and Phar ma codyna mi cs – Rout e of admi nist rati on – Abs orption – Met abol is m – Eli mi nati on – Non li nea r a nd ti me de pe ndent pha r ma coki net ics .

Unit 2: P ri nci pl es of The rape ut ics

De finiti on and e xpl ana tion of M EC, M SC, M PC, AV C ( gra ph), LD50, ED50 a nd T her apeutic Index.

Unit 3: P ri nci pl es of dr ug di sc over y

Dr ug dis cover y wi thout Le ad – Le ad di scove r y – Ra ndom s c ree ni ng – Non r andom s c re ening – Cli ni cal obse r vati on- Phas e I, Phas e II, Phas e III a nd Phas e IV t rai ls .


Pri nci pl es of dr ug des i gn : Defi niti on –Agoni st – Ant a goni st drugs – de vel opme nt of c i met idine fr om Lea d mol ecule s.

M ol ec ular modeli ng – Ener gy mi ni mi zat ion – ener gy c alc ul ati on.

Unit 4: SAR and Q SAR Rel ati ons hi p

SAR : Defi nit ion – Bindi ng of hydr oxyl gr oup, a mi no gr oup, aroma t ic ri ng of ke t ones .

Va ria tion s ubstit ue nt s : Al kyl s ubstit uent s, Ar oma tic s ubsti tuent s, Is os ter es .

QSAR: Defi nit ion – Pa ra me te rs – e lec tr oni c para me t ers – St eri c pa ra me te rs .

Unit 5: P harm ac ologic al s cr ee ni ng m et hodology of dr ug

Anal ge sic ac ti vit y – CNS st i mula nt – CNS de pr ess ant – Ant i i nf la mma t or y – Antic onvuls ant – Musc le re la xa nt proper tie s.

Ref e re nc es : 1. Goodman and Gilman's “The Pharmacological Basis of Therapeutics”, Gilman, Joel G.Hardman, Lee.E.Limbird, 5 t h Edn., 2001. 2. Biopharmaceutics and Pharmacokinetics, D.M.Brahmanikar and Sunil B. Jaiswal, Edn. XIX 2004. 3. Pharmacology, Mary J.Mycek and Richard A. Harvey 2 n d Edn. 2000. 4. Foye's principles of medicinal chemistry, A.Williams and Thomas L.Lemke, Edn. V, 2002.



5. Pharmacology and Pharmacotherapeutics, R.S.Staskar, S.D.Bhandakar and S.Ainapure, Edn. XVIII, 2003. 6. Hand book of Experimental Pharmacology, S.K.Kulkarni, 3 r d Edn., 1999. Paper 4 Synthesis and Therapeutic action of drugs

Unit 1 : Anti i nf lamm at or y, Anal ge si c and Ant i pyre tic dr ugs

Synt he sis and t he ra peutic ac tion of As pir in, Par ac eta mol , Anal gin, Ibuprofe n, Indome t haci n, and Dicl of enac s odi um.

Unit 2 : Chem ot he rape uti c age nt s


Cl ass ifi cati on – Synt he si s a nd t he ra pe uti c ac tion of c hl ona mbucil, Busul fa n, 6 – me rc a ptopuri ne , 5 – f luor our ac il and ci spla tin.

Anti ma lar ial , Antit ube rc ula r dr ugs : Synt he sis and ther apeuti c ac tion of Et ha ma butol, Et hionami de , c hloroquine, and pri ma qui ne .

Unit 3: Ant ihype rte ns ive and Di ur eti cs drugs

Anti hyper te nsi ve dr ugs : Synt he si s a nd t he ra pe uti c ac tion of c aptopril , me t hyl dopa , a nd nife di pi ne .

Di ure tic s; Synthesi s and ther apeut ic ac tion of Fure se mi de, Chl orothia zide and bul me t ani de .

Unit 4 : Anti hi st ami ne s , CNS sti mulant and CNS de pr ess ant drugs

Anti hist a mi ne s: Synthes is and t he ra pe uti c prome t ha zine , ci me tidi ne a nd r a niti di ne .

a cti on


c hl orpheni ra mi ne ,

CNS s ti mula nt : Synthes is a nd thera pe ut ic a cti on of caf fei ne , theobr omi ne a nd pir ace ta m.

CNS depre ssa nt : Synt he si s De si pra mi ne and tr a zodone .

a nd

ther ape utic

a cti on


Is oc ar boxa zi d,

Unit 5: Chemic al assay

Che mi cal as sa y of As pir in, 6-me r ca ptopuri ne , r anidi tine, f ur esi mi de a nd theobr omine .

c hl or oqui ne,

me t hyldopa ,

Ref e re nc es: 1. Be ntl y&a pos; s te xt of Phar ma ce uti cs , E.A.Ra wlins , 8 t h Edn.2002. 2. Pri nci pl es of me dici nal c he mi st r y, S.S.K adam, K .R. Ma ha di k, K .G.Bot har a, V ol.I 10 t h Edn., 2002. 3. Pri nci pl es of me dici nal c he mi st r y, S.S.K adam, K .R. Ma ha di k, K .G.Bot har a, V ol.II, 10 t h Edn.,2002. 4. Sci ence a nd pr acti se of phar ma c y, Re mi ngton, Vol. I a nd V ol .II, 20 t h Edn.,2000 5. M edici nal Che mi str y, G.R.Chat wal , Hi ma l a ya Publi shing Hous e, 2 n d Edn. 2002. 6. Phar ma c ology a nd phar ma c ot her apeutic s, R.S. Sat as ka r, S.D.Bha nda nkar a nd S.S.Ai na pure , 2003 7. Int r oducti on t o me dicinal c he mi st r y, Gra ha m L.Pat ric k 2 n d Edn., 2003.


Paper 5 Industrial Processes in Drug Manufacture Unit 1: Industrial drug manufacture l introduction – Raw materials – Manufacturing Procedure – therapeutic function – common name – Structure of naproxen, acyclovir, propanolol, and levodopa. Unit 2: Industrial drug manufacture II Introduction – Raw materials – Manufacturing Procedure – therapeutic function – common name – Structure of mephensin, 5-fluorouracial levothyroxin sodium amoxycillin, and norfloxacin. Unit 3: Industrial manufacturing of tablets, ointments and suspension Tablet: Raw material – Flow chart diagram – Manufacturing processes. Ointments : Raw material – Flow chart diagram – Manufacturing processes. Suspension : Raw material – Flow chart diagram – Manufacturing processes. Unit 4: Industrial unit processes Introduction – alkylation – amination – Nitration – Oxidation – Halogenation. Unit 5 : Industrial hazards and safety measures Hazards – Definition – Chemical hazard – Dust hazard – Electrical hazar-Preventive measures – Use of PPE. References: 1. 2. 3. 4.

industrial Chemistry, B.K.Sharma.Goel publishing house,Edn.XIV,2004. Unit processes in organic synthesis, Groggins,5th Edn.,2000. Pharmaceutical manufacturing encyclopedia ,Vol.l and II,2nd Edn.,2001. Biopharmaceutics and. Pharmacokinetics, D.M.Brahmanikar and Sunil B.Jaiswal, Edn.XIX 2004. 5. Pharmaceutical analysis , Takeru Higuchi, Einar Brochmann and Hanffen Hanseen, 3rd Edn.2004.