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7-Endo-trig Pictet–Spengler type cyclization of 5-alkylidene/arylidene-amino-3H-pyrimidin-4-ones: An efficient and diastereoselective synthesis of pyrimido[4,5-b] [1,4]benzodiazepines.
- Source :
-
Synthetic Communications . 2021, Vol. 51 Issue 8, p1232-1241. 10p. 8 Diagrams, 2 Charts. - Publication Year :
- 2021
-
Abstract
- The manuscript describes an efficient, atom economical synthesis of pyrimido[4,5-b][1,4]benzodiazepin-4-ones by relatively unexplored 7-endo-trig Pictet–Spengler type cyclisations. The synthetic methdodlogy involves the synthesis of different variants of 5-arylidene-amino-3H-pyrimidines and their p-toluene sulfonic acid mediated 7-endo-trig Pictet–Spengler type cyclisations to afford biologically relavent functionalized benzodiazepine condensed pyrimidinones such as pyrimido[4,5-b][1,4]benzodiazepines in good to excellent yields (82–94%). [ABSTRACT FROM AUTHOR]
- Subjects :
- *BENZODIAZEPINES
*RING formation (Chemistry)
*SULFONIC acids
Subjects
Details
- Language :
- English
- ISSN :
- 00397911
- Volume :
- 51
- Issue :
- 8
- Database :
- Academic Search Index
- Journal :
- Synthetic Communications
- Publication Type :
- Academic Journal
- Accession number :
- 149223205
- Full Text :
- https://doi.org/10.1080/00397911.2021.1878224