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Indian Journal of Chemistry

Sect. B: Organic Chemistry including Medicinal Chemistry

 

 

 

VOLUME 44 B

NUMBER 2

FEBRUARY 2005

 

 

CONTENTS

 

Rapid Communications

 

 

 

327

A convenient, rapid and eco-friendly synthesis of bis-indolylmethanes under microwave irradiation

 IPC: Int.Cl.7 C 07 D 209/04

 

 

 

Biswanath Das*, Rammohan Pal, Joydeep Banerjee, Chimmani Ramesh, Gurram Mahender & Katta Venkateswarlu

 

 

 

 

 

 

 

331

Chemoselective tetrahydropyranylation of primary alcohols under freezing water pressure

 IPC: Int.Cl.7 C 07 D 309/00

A highly efficient environmentally friendly method for selective tetrahydropyranylation of primary alcoholic groups under pressure exerted by freezing water has been described.

 

 

Joshodeep Boruwa, Ranjana Bhuyan, Naminita Gogoi & Nabin C Barua*

 

 

 

 

Advances in Contemporary Research

 

 

 

335

Combinatorial chemistry: A novel method in drug discovery and its application

 

IPC: Int.Cl.7 A 61 P // C 07 K

Combinatorial chemistry is a new technique developed in pharmaceutical industry, which involves synthesis of compounds in mass instead of a single compound, which are screened as a whole mixture for particular biological activity. This brief review article includes combinatorial strategies, screening methods and encoding technologies and some of the applications in drug discovery.

 

 

S N Pandeya & D Thakkar*

 

         
Papers

 

 

 

349

Preparation of carbamate modified alumina supported heterobinuclear macrocyclic cobalt/
vanadium complex for n-octane oxidation reaction

 IPC: Int.Cl.7 C 07 C 9/14

A binuclear macrocyclic complex CoII VIV L2+ bonded to carbamate modified alumina is used as a catalyst for oxidation of n-octane which gives oxidative products, 2-octanone, 3-octanone, octanol and octanoic acid without any isomerization or cracking products.

 

 

M Jhansi, L Kishore, G S Mishra & Anil Kumar*

 

 

 

 

 

 

356

Candida rugosa lipase-mediated enantioselective acetylation studies on (±)-3-arylmethyl-3-hydroxymethyl-2,3-dihydro-1-benzopyran-4(H)-ones

 IPC: Int.Cl.7 C 07 D 311/04

Candida rugosa lipase catalyzed enantioselective acetylation reactions have been performed on novel (±)-3-arylmethyl-3-hydroxymethyl-2,3-dihydro­ben­zo­pyran-4(H)-ones in diisopropyl ether.

 

 

Smriti Trikha, Rajesh Kumar, Ashish Dhawan, Poonam, Ashok K Prasad, Ashok L Cholli, Carl E Olsen, Arthur C Watterson & Virinder S Parmar*

 

 

 

 

 

 

366

Synthesis of syn-N-arylsulfonyl-4-substituted phe­nyl-2-oxo-1,3-oxazolidine-5-carboxylates and their conversion to anti- form using DBU

 

IPC: Int.Cl.7 C 07 D 263/00 // A 61 P 31/04

Novel syn-N-arylsulfonyl-4-substituted phenyl-2-oxo-1,3-oxazolidine-5-arboxylates have been synthesized from the corresponding b-azido alcohols and converted to their anti- form by epimerizing C-2 proton using DBU. Studies on the stabilization energies are done to evaluate conversion from syn- to anti- and not the vice-versa. All the compounds have been tested for their in vitro anti-bacterial activity against S.aureus, E.faecalis and E.faecium.

 

 

 

G Madhusudhan, G Om Reddy*, J Ramanatham & P K Dubey

 

 

 

 

 

 

372

A facile synthesis of di-O-methyl centrolobol

 IPC: Int.Cl.7 C 07 D 309/00

A convenient synthesis of di-O-methyl centrolobol 4 has been achieved using readily available precursors.

 

 

Atulya Kumar Panda

 

 

 

 

 

 

 

376

Microwave-assisted synthesis of some new isoxazolyl-[1,3,5]-triazinan-2-ones and isoxazolyl-[1,3,5]-oxadiazinan-4-ones in dry media

 

IPC: Int.Cl.7 C 07 D 251/00, 261/00

Trimolecular condensation of N-(3-methyl-5-styryl-4-isoxazolyl)-N'-aryl ureas 2, paraformaldehyde and primary amines using montmorillonite K-10 in dry media under microwave irradiation leads to isoxazolyl-[1,3,5]-triazinan-2-ones 3 in high yields. Condensation of 2 with paraformaldehyde under similar conditions provides isoxazolyl-[1,3,5]-oxadiazinan-4-ones 4 in excellent yields.

 

 

 

 

E Rajanarendar*, Md Afzal & K Ramu

 

 

 

 

 

 

 

381

Studies on the reactivity pattern of in situ generated tetraethylammonium superoxide with 2-oxazolin-5-ones

IPC: Int.Cl.7 C 07 D 263/00

 

 

 

Krishna Nand Singh* & Rajesh Kumar

 

 

 

 

 

 

 

387

Synthesis, hydrolysis over silica column, anticancer, anti-inflammatory and analgesic activity evaluation of some pyridine and pyrazine derivatives

IPC: Int.Cl.7 C 07 D 211/00, 231/00 //A 61 P 35/02, 29/00, 25/04

 A number of pyridine and pyrazine derivatives have been synthesized and evaluated for anticancer, anti-inflammatory and analgesic activities.

 

 

  

 

Sham M Sondhi*, Nirupma Singh, Shefali Rajvanshi & Monika Johar, Rakesh Shukla, Ram Raghubir & Sunanda G Dastidar

 

 

 

 

 

 

400

Isolation, antihypertensive activity and structure activity relationship of flavonoids from three medicinal plants

 

IPC: Int.Cl.7 C 07 D 311/30

Eight flavonoids, namely naringenin 1, isoaromadendrin 2, taxifolin 3, isosinensin 4 have been isolated from Euphorbia cuneata Vahl; 5-hydroxy- 3, 4′, 7- trimethoxyflavone 5, retusin 6, verbenacoside 7 from Salvia verbenaca L; and epicatchin 8 from Osyris abyssinica. The compounds 2, 4 and 7 are found to be new flavonoids. They are screened for antihypertensive activity. The SAR has also been discussed. 

 

   

 

Bahar Ahmed*, Tawfeq A Al-Howiriny, Jaber S Mossa & K E H EL Tahir

 

 

 

 

 

 

 

 

 

405

Facile synthesis of some new azetidinones and acetyl oxadiazoles bearing benzo[b]thiophene nucleus as a potent biological active agent

 

IPC: Int.Cl.7 C 07 D 333/52 // A 61 P 31/06, 31/04

Acetyl oxadiazoles 4a-l and 2-azetidinones 3a-l have been synthesized by the cyclocondensation of schiff bases 2a-l. Compound 2a-l have been synthesized from the reaction of 2-hydrazinocarbobyl-3-chloro-5-phenoxybenzo[b]thiophene with hydra­zine hydrate. All the compounds are screened for their anti­tubercular and antimicrobial activities.

 

 

 R=Aryl

 

S L Vasoya, M R Patel, S V Dobaria & H S Joshi*

 

 

 

 

 

 

 

410

Synthesis and pharmacological evaluation of
2-(3
, 5-dichlorobenzo[b]thiophen-2-yl)-5-aryl­ami­no-1,3,4-thiadiazoles

 

 

IPC: Int.Cl.7 C 07 D 285/12

The condensation of 2-hydrazinocarbonyl-3,5-dichloro­benzo[b]thiophene 1 with different aryliso­thiocyanate yields N1-(3,5-dichlorobenzo­[b]­thio­phen-2-yl)-N4-substituted arylthiosemicarbazides 2a-j. Reaction of 2a-j with conc. H2SO4 affords the corres­ponding 2-(3,5-dichlorobenzo[b]thiophen-2-yl)-5-arylamino-1,3,4-thiadiazoles 3a-j. The pharma­co­logical evaluations have been performed for their antimicrobial and antitubercular activities. 

 

 

 

K M Thaker & H S Joshi*

 

 

 

 

Notes

 

 

 

413

Synthesis of 5,6,7,3'-tetramethoxy-4'-hydroxy-8-C-prenylflavone

 IPC: Int.Cl.7 C 07 D 311/30

5,6,7,3'-Tetramethoxy-4'-hydroxy-8-C-prenylflavone 5 has been synthesized  from the 2,4,5,6-tetrahydroxy-
 acetophenone 1.

 

 

M Amzad Hossain* & Zhari Ismail

 

 

 

 

 

 

 

416

Microwave assisted synthesis of 4-alkyl-2-([5-substituted-2-hydroxyphenyl]­iminomethyl)­benze­nols and their NMR characterization

 IPC: Int.Cl.7 C 07 C 47/228, 39/00

Imines, 4-alkyl-2-([5-substituted-2-hydroxyphenyl]­imino­­methyl)benzenols 1, have been obtained succes­s­fully in excellent yield from the corresponding aldehydes and amines by microwave irradiation. The resultant Schiff bases have been fully characterized by spectral data.

 

 

 

V Sridharan, S Muthusubramanian* & S Sivasubramanian

 

 

 

 

 

 

 

420

Synthesis of anhydrides from acyl halides and zinc carboxylates under aprotic conditions

 IPC: Int.Cl.7 C 07 C 53/00

Synthesis of symmetric as well as unsymmetrical carboxylic acid anhydrides from zinc carboxylates and acid chlorides under aprotic conditions in high yields, is reported.

 

 

 

M A Pasha* & S Rizwana

 

 

 

 

 

 

 

422

Synthesis, characterization and antimicrobial activities of some fluorinated compounds

 

IPC: Int.Cl.7 C 07 D 231/00 // A 61 P 31/04, 31/10

Compound 3 on oxidative cyclization with DMSO-CuCl2 and DMSO-I2 gives 2-(1-phenyl-3-aryl-1H-pyrazol-4-yl)-3-chloro-6-flurochromones 4 and (1-phenyl-3-aryl-1H-pyrazol-4-yl)-6-flurochromones 5, res­­pecti­vely. 3 when heated with hydrazine in dioxane gives [5-(1-phenyl-3-aryl-1H-pyrazol-4-yl)-3-(5-fluoro-2-hy­dro­xy­phenyl)-4,5-dihydropyrazolines 6.

 

 

N S Joshi, A A Shaikh, A P Deshpande, B K Karale, S B Bhirud & C H Gill*

 

 

 

 

 

 

 

426

A novel route to anticonvulsant imesatins and an approach to cryptolepine, the alkaloid from Cryptolepis Sp.

 

IPC: Int.Cl.7 C 07 D 209/04

Interesting products having anticonvulsant properties are synthesized from solution phase dielectric heating of isatin and aromatic amines and diamines without any catalyst and an approach to cryptolepine is made from one of them. In addition, the crystal structure of the condensation product between isatin and a diamine is reported.

 

 

J Banerji*, T K Lai, B Basak, A Neuman, T Prange & A Chatterjee*

 

 

 

 

 

 

 

430

Studies on the chemical constituents of Nardo­stachys jatamansi DC (Valerianaceae)

 IPC: Int.Cl.7 A 61 K 35/00

A new sesquiterpene acid 1 and a new pyrano­coumarin 2 have been isolated from the rhizomes of Nardostachys jatamansi. Their structures have been established from spectral and X-ray crystallographic studies and chemical correlation.

 

 

A Chatterjee*, B Basak, U Datta, J Banerji*,
A Neuman & T Prangé

 

 

 

 

 

 

 

 

434

2-Methylhexadec-2-ene from Phyllanthus  niruri Linn.

 IPC: Int.Cl.7 A 61 K 35/00

2-Methylhexadec-2-ene 1 has been  isolated from farm-grown  Phyllanthus  niruri Linn. Its structure has been determined by IR, 1H NMR and mass spectroscopic methods.

 

 

 

Rumi Kotoky  & Purnendu B Kanjilal & Manobjyoti Bordoloi*

 

 

 

 

 

 

 

436

A new lupene–type triterpene from the leaves of Orthosiphon stamineus

 IPC: Int.Cl.7 C 07 C 15/20 // A 61 K

Orthosiphonoic acid 1 has been isolated and identified from the leaves of local Orthosiphon stamineus

 

 

M Amzad Hossain* & Zhari Ismail

 

 

 

 

 

 

 

438

Additions and Corrections

 

 

 

Authors for correspondence are indicated by (*)

IPC: International Patent Classification

Int. Cl7.: International Classification 7th  edition, 1999