Solid-phase synthesis of disubstituted guanidines
โ Scribed by Patrick C. Kearney; Monica Fernandez; John A. Flygare
- Publisher
- Elsevier Science
- Year
- 1998
- Tongue
- French
- Weight
- 227 KB
- Volume
- 39
- Category
- Article
- ISSN
- 0040-4039
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โฆ Synopsis
A method for the solid-phase synthesis of disubstituted guanidines is reported. In this procedure, polymer-bound aryl or alkyl amines are converted to methyl isothioureas in three steps and treated with primary and secondary amines to form the disubstituted guanidine products.
๐ SIMILAR VOLUMES
The solid-phase synthesis of trisubsituted guanidines is reported via aza-Wittig coupling of a solid-supported alkyl iminophosphorane with an aryl or alkyl isothiocyanate to generate the corresponding solid-supported carbodiimide which is then reacted with a primary or secondary amine to afford the
An efficient method for the solid-phase synthesis of substituted guanidines is presented. A variety of alcohols react with resin-bound N,N'-bis(t-butoxycarbonyl)thiopseudourea under Mitsunobu conditions to give the corresponding alkylated thiopseudoureas. The guanidines are liberated from the resin
A novel linker for the generation of alkyl-, acyl-and arylguanidines as an attachment point in solid phase synthesis has been developed. Introduction of a suitably functionalized thiourea to Wang resin via a carbamate linkage, followed by displacement of sulfur with a 1 ยฐ or 2 ยฐ amine affords resin