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Indian Journal of Chemistry

Sect. B: Organic Chemistry including Medicinal Chemistry

 

 

 

VOLUME 43 B

NUMBER 7

JULY 2004

 

 

CONTENTS

Rapid Communications

1485

Tin (II) chloride catalyzed one pot efficient and novel preparation of dihydropyrimidin-2(1h)-ones

 

IPC: Int.Cl.7 C 07 D 239/00, C 07 G 19/04

A new method for the preparation of dihydro­pyrimidin-2(1H)-ones is reported using tin chloride dihydrate as mild Lewis acid catalyst in one pot three component coupling reaction of 1,3-diketones, alde­hydes and urea.

Sanjay Kumar, Anil Saini & Jagir S Sandhu*

 

Papers

1487

 

 

[1,2-Bis (salicylideneamino)phenylene] cobalt (II) complex supported on carbamate modified silica gel as a reformation catalyst for n-hexane

 

IPC: Int.Cl.7 C 07 C 9/00

Gopal S Mishra, Amit Kumar & Anil Kumar

1493

 

 

 

 

 

Synthesis and characterization of drum clusters hexameric benzyloxotin aromatic substituted acrylates and crystal structure of hexameric benzyloxotin cinnamate

 

IPC: Int.Cl.7 C 07 C 57/44, 57/04

The seven drum hexameric benzyloxotin aromatic substituted acrylates are synthesized by the reaction of [(PhCH2)3Sn]2O with aromatic substituted acrylic acids in 1:2 molar ratio. The crystal structure of hexameric benzyloxotin cinnamate is determined by X-ray single crystal diffraction.

Handong Yin*, Chuanhua Wang & Yong Wang

 

1499

Synthesis of cyclophanes bearing 1,4-dioxabut-2-yne and 1,6-dioxahexa-2,4-diyne bridges and nanoscale cavities

 

IPC: Int.Cl.7 C 07 C 43/20

Synthesis and structure of cyclophanes having nanoscale cavities based on bisphenol-A is reported.

Sethuraman Sankararaman*,Manivannan Srinivasan, Vijay Narayanan & Babu Varghese

 

1504

Correlation between vapour pressure of organic compounds and semiempirical theoretical descriptors

 

 

 

IPC: Int.Cl.7 C 07 C 321/00

A quantitative structure-property treatment of vapour pressure has been performed for a structurally wide variety of organic compounds using theoretical descriptors, which are calculated by semiempirical molecular orbital methods (MNDO and AM1 algorithm). The suggested multi-parameter equations are statistically acceptable.

 

Aziz Habibi Yangjeh

 

 

1527

Synthesis and acidic properties of some new  potential biologically active 4-acylamino-4,5-dihydro-1H-1,2,4-triazol-5-one derivatives

 

IPC: Int.Cl.7 C 07 D 249/08

Ten new 3-alkyl(aryl)-4-acylamino-4,5-dihydro-1H-1,2,4-triazol-5-ones have been synthesized and solutions of these compounds  are titrated potentio­metrically with tetrabutylammonium hydroxide in four non-aqueous solvents. Thus, the pKa values of these compounds are determined.

Haydar Yüksek*, Muzaffer Alkan, Zafer Ocak, Şule Bahçeci, Miraç Ocak & Mustafa Özdemir

 

1532

Synthesis of anti-inflammatory, analgesic and COX-II inhibitory activities of indolyl­pyrazolines

 

 

IPC: Int.Cl.7 C 07 D 209/04 // A 61 P 29/00

Some 1-[N-phenylsulphonyl-3-(2'-substituted-3'-sul­pho­­nyl-5'-methoxy­indol-3'-yl)]-2-pyrazolines 7-8 and 1-[N-benzoyl-3-(2'-substituted-3' sulphonyl-5'-me­thoxy­indol-3yl)]-2-pyrazolines 5-6 have been synthesized and evaluated for anti-inflammatory, analgesic and COX-II inhibitory activities.

Ashok Kumar*, Archana, Shalabh Sharma, Nidhi Malik, Preeti Sharma, Kavita Kaushik, Kuldeep Kumar Saxena, Virendra Kishore Srivastava, R S Verma, Himansahu Sharma, S C Gupta, Vipul Gupta & R C Agarwal

 

1537

Synthesis of naphtho[2,1-b]furo[3,2-e]-1,4-diaze­pin-2-ones and naphtho[2,1-b]furo[3,2-e]-1,3,4-triazepin-2-ones of pharmacological interest

 

IPC: Int.Cl.7 C 07 D 241/00 // A 61 P 29/00, 31/04, 31/10, 33/10

Naphtho[2,1-b]furo[3,2-e]-1,4-diazepin-2-ones and naphtho[2,1-b]furo[3,2-e]-1,3,4-triazepin-2-ones have been synthesized from suitably 2,3-disubstituted naphtho[2,1-b]furans. The newly synthesized compounds have been evaluated for antimicrobial, anthelmintic and analgesic activities.

V P Vaidya*, H M Vagdevi, K M Mahadevan & C S Shreedhara

 

1544

Synthesis of biologically active N-[coumarin-6-yl]-3-methyl-5-(hydroxy/methyl/4-hydroxy-8-me­thyl­coumarin-3-yl)pyrazoles and [2.3.1]-bicyclo-N-[coumarin-6-yl]-1,2-diazepines

 

IPC: Int.Cl.7 C 07 D 231/00, C 07 D 243/00 

Synthetic utility of 1 to synthesise biologically active N-[coumarin-6-yl]-5-hydroxy-3-methylpyrazole 3, N-[cou­marin-6-yl]-3,5-dimethylpyrazole 4, N-(cou­m­arin-6-yl)-3-methyl-5-(4-hydroxy-8-methylcoumarin-3-yl)pyrazole 5 and [2.3.1]-bicyclo-N-(coumarin-6-yl)-4H-5,6-dihydro-1,2-diazepine 6 has been described.

B P Choudhari & V V Mulwad*

 

1548

An elegant synthesis of quino[2,3-a]carba­zoles and their antibacterial studies

IPC: Int.Cl.7 C 07 D 209/82 // A 61 P 31/04

Synthesis of new quino[2,3-a]carbazoles is reported by the reaction of 1-oxo-1,2,3,4-tetrahydrocarbazoles 1 with o-aminobenzonitrile 2 in toluene.

I Antony Danish & K J Rajendra Prasad*

 

1553

Synthesis and anti-hypertensive activity of some dihydropyrimidines

 

 

 

IPC: Int.Cl.7 C 07 D 239/00 // A 61 P 9/12

Acetoacetic ester, thiourea and substituted aldehydes are condensed to give tetrahydropyrimidines deri­vatives which subsequently react with alkyl sulphates and alkyl chlorides to give dihydropyrimidines. These compounds show good anti-hypertensive activity and show some new results about the structure-activity relationship contrary to an earlier reports.

Kulbhushan Rana, Balbir Kaur &

Baldev Kumar*

1558

Aminoimidazoliumcarboxamide with dimethyl­formamide - dimethylacetal: A novel ANRORC towards rearranged imidazole anchored with one-carbon fragment

 

IPC: Int.Cl.7 C 07 D 233/54

Aminoimidazoliumcarboxamides 1 with DMF-DMA affords 4-(N-aryl-N-substituted methyl)amino-1-methyl­I­midazole-5-caboxamide 2. 4-(N-Benzyl-N-substi­tuted methyl)­amino-1-methylimidazole-5-cabox­amide 2a on warming with aq.HCl yields 3-benzyl-7-methylpurin-6(3H)-one 3a.

R = benzyl, phenyl, allyl, p-tolyl, p-chlorophenyl

Gautam Chattopadhyay* & Tapas Kumar Saha

 

1561

Cyclocondensation of cyanoketene dithio­acetal with 2-aminopyridine : Synthesis of pyrido [1, 2-a]pyrimidines

 

 

 

 

IPC: Int.Cl.7 C 07 D 239/00

The cyanoketene dithioacetal l on reaction with 2-aminopyridine gives 2-methylthio-3-cyano-4-H-pyrido [1, 2-a] pyrimidines 3 in good yield which on reaction with primary amines yields 2-amino-3-cyanopyrido[1,2-a]pyrimidin-4(H)-ones 4a-d is further converted to tricyclic compounds 5,6 and 7 by reacting with hydrazine hydrate, hydroxylamine and guanidine nitrate, respectively.

Okram Mukherjee Singh* & Mohd Farooque Ahmed

 

1565

Microwave assisted synthesis of 1-methyl-5-aryl-3-[(E)-2-arylethenyl]-4,5-dihydro-1H-pyra­­zoles and 2-methyl-3-aryl-7-[(E)-aryl­methyl­idene]-3,3a,4,5,6,7-hexahydro-2H-indazoles

 

IPC: Int.Cl.7 C 07 D 231/00

A solventless and expeditious method for the synthe­sis of 1-methyl-5-aryl-3-[(E)-2-arylethenyl]-4,5-di­hydro-1H-pyrazoles and 2-methyl-3-aryl-7-[(E)-aryl­methylidene]-3, 3a, 4, 5, 6,7-hexahydro-2H-indazoles from the reaction of diarylideneacetones and diaryl­idenecyclohexanones respectively with methyl­hydrazine under microwave irradiation is reported.

E Karthikeyan, S Perumal* & S Selvaraj

 

1569

 

Studies on biological evaluation of cyano­pyrans and pyrazolines using microwave assisted synthesis

 

IPC: Int.Cl.7 C 07 D 309/00

 

Text Box: 2a-k

Text Box: 4a-k
R=Aryl

1574

Synthesis and hypotensive activity of some 6-(substituted aryl)-4-methyl-2,3-dihydropyrid­azin-3-ones

 

IPC: Int.Cl.7 C 07 D 237/00 // A 61 P 9/02

A series of 6-(substituted aryl)-4-methyl-2,3-dihydro­pyrid­azin-3-ones has been synthesized which show significant hypotensive activity.

 

  Anees A Siddiqui* & Sachin M Wani

1580

Synthesis of chalcones, pyrazolines, aminopyr­imidines and pyrimidinethiones as antibacterial agents

 

 

 

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

2 - Phenylamino-4-(3'-fluorophenylamino) –6-(4'-acetyl­­phenyl­­amino)-s-triazine 5 on treatment with aromatic aldehydes yields chalcones 6a-f, which on cyclization with hydrazine hydrate, guanidine nitrate and thiourea give the corresponding pyrazolines 7a-f, aminopyri­midines 8a-f and pyrimidinethiones 9a-f, respectively. The synthesized compounds are screened for their antibacterial activity.

 

 

Anjani Solankee* &  Jayesh Patel

 

 

1585

Heterocyclic systems containing bridgehead nitrogen atom: Synthesis and bioactivity of thi­azolo[3',2':2,3]-as-triazino[5,6-b]indoles and iso­meric thiazolo[2',3': 3,4]-as-triazino[5,6-b]indoles

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

Synthesis of  3-(p-bro­mobenzoyl)-7-isopropylthiazolo- [3', 2': 2,3]-as-triazino[5,6-b] indoles 9 and its isomer 1-(p-bromo-7-isopropylthiazolo[2',3':3,4]-as-tri­a­zino [5,6-b]indole 6 have been achieved. Their ant­ibacte­rial and antifungal activity have also been evaluated.

 

  

  Jag Mohan

1588

Additions and Corrections

 

 

 

 

Authors for correspondence are indicated by (*)

                   IPC: International Patent Classification

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