A versatile method for the solid phase synthesis of oxazolidin-2-ones is described. A resin bound phenolic group was treated with (ยฑ)-epichlorohydrin followed by opening of the epoxide ring with sodium azide. The resulting 1-azido-3-aryloxypropan-2-ol was treated with p-nitrophenylchloroformate and
โฆ LIBER โฆ
Solid-phase synthesis of 3,5-disubstituted 1,3-oxazolidin-2-ones by an activation/cyclo-elimination process
โ Scribed by Peter ten Holte; Lambertus Thijs; Binne Zwanenburg
- Book ID
- 108387037
- Publisher
- Elsevier Science
- Year
- 1998
- Tongue
- French
- Weight
- 183 KB
- Volume
- 39
- Category
- Article
- ISSN
- 0040-4039
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We have developed a solid-phase synthesis of diverse 1,3-disubstituted 2-thioxoquinazoline-4-ones. In this synthesis, the fluorine atom on support-bound 2-fluoro-5-nitrobenzoyl amides was substituted with various primary amines, followed by cyclization with thiocarbonyldiimidazole. Since 1-substitut