Synthesis of Biologically Active Pyridoimidazole/Imidazobenzothiazole Annulated Polyheterocycles using Cyanuric Chloride in water
IR@CDRI: CSIR-Central Drug Research Institute, Lucknow
View Archive Info| Field | Value | |
| Creator |
Pandey, A K
Sharma, Rashmi Singh, Awantika Shukla, Sanjeev Srivastava, Kumkum Puri, S K Kumar, Brijesh Chauhan, P M S |
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| Date |
2014-09-19T08:43:07Z
2014-09-19T08:43:07Z 2014 |
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| Identifier |
RSC Advances, 2014, 4, 26757-26770
http://hdl.handle.net/123456789/1410 |
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| Description |
An efficient and mild protocol for rapid access to N-fused polyheterocycles via Pictet-Spengler type 6-endo cyclization using cyanuric chloride in aqueous reaction medium has been developed. The protocol is successfully applied to a wide range of aryl/heteroaryl aldehydes (8a-o), ketones (10a-e), electron rich metallocene aldehyde (8e) and indoline-2,3-diones (12a-c) using cyanuric chloride (15-20 mol %) with tetra-n-butylammonium bromide (TBAB) (2.0 equiv.) as an additive at 80-90 ˚C to give polyheterocycles in good to excellent yield (66-92%). Moreover some of the synthesized compounds were found to exhibit antiplasmodial activity against chloroquine sensitive (CQ-S) 3D7 and chloroquine resistant (CQ-R) K1 strains of Plasmodium falciparum.
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| Format |
391326 bytes
application/pdf |
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| Language |
en
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| Relation |
CSIR-CDRI Communication No. 8715
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| Subject |
Cyanuric Chloride
Heterocycles Imidazobenzothiazole Pictet-Spengler Reaction Pyridoimidazole Tetra-N-Butylammonium Bromide (TBAB) |
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| Title |
Synthesis of Biologically Active Pyridoimidazole/Imidazobenzothiazole Annulated Polyheterocycles using Cyanuric Chloride in water
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| Type |
Article
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