New thiazolo[3,2-a]pyrimidine derivatives, synthesis and structure-activity relationships
β Scribed by E Jeanneau-Nicolle; M Benoit-Guyod; A Namil; G Leclerc
- Publisher
- Elsevier Science
- Year
- 1992
- Tongue
- French
- Weight
- 523 KB
- Volume
- 27
- Category
- Article
- ISSN
- 0223-5234
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π SIMILAR VOLUMES
An efficient one-pot method to synthesize thiazolo[3,2-a]pyrimidine derivatives has been developed. The method involves the temperature controlled functionalization-annulation of 5-ethoxycarbonyl-6methyl-4-aryl-3,4-dihydro-2(1H)-pyrimidin-2-thione (DHPM) derivatives with in-situ generated bromo-keto
Reaction of 2-aminothiazoline (1) with a,b-unsaturated carbonyl compounds 2 under mild conditions (acetone, room temperature) gives two diastereomers 5-R-7-hydroxy-5H-tetrahydrothiazolo[2,3-a]pyrimidines 3. According to 1 H NMR, major isomers of 3 have axial OH-groups whereas minor isomers have equa