A new method for the solid phase synthesis of benzothiazoles and 2-arylamino-3-carboxyl-4-hydroxy-5-arylthiophenes is described. Resin bound cyclic malonic acid ester was reacted with aryl isothiocyanates and then with bromine or a-bromoketones, followed by treatment with perchloric acid or sodium m
Preparation of a resin-bound cyclic malonic ester and a facile solid-phase synthesis of 4(1H)quinolones
β Scribed by Xian Huang; Zhanxiang Liu
- Publisher
- Elsevier Science
- Year
- 2001
- Tongue
- French
- Weight
- 61 KB
- Volume
- 42
- Category
- Article
- ISSN
- 0040-4039
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β¦ Synopsis
A resin-bound cyclic malonic ester has been prepared on Merrifield resin. Reaction of the cyclic malonic ester with triethyl orthoformate and subsequent substitution by an arylamine afforded arylaminomethylene cyclic malonic ester preloaded resin. A series of 4(1H)quinolones were prepared by thermal cyclization in moderate yields and high purity.
π SIMILAR VOLUMES
## a-Amidoalkylation Partial hydrolysis Solid-phase peptide synthesis a b s t r a c t MBHA (4-methylbenzhydrylamine) resin has been extensively used as a solid support for the synthesis of peptide amides. Herein, we prepared the core-shell-type MBHA resin by benzotriazole-catalyzed amidoalkylation