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Solid-phase synthesis of PhTX-3.2.4 and PhTX-2.3.3 derivatives

✍ Scribed by Daniel Jönsson

Publisher
Elsevier Science
Year
2002
Tongue
French
Weight
208 KB
Volume
43
Category
Article
ISSN
0040-4039

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✦ Synopsis

A new solid-phase method for the synthesis of derivatives of the philanthotoxins is described. Diamines are attached as carbamates to hydroxymethyl polystyrene resin. Selective mono-alkylations by acid-labile, substituted benzhydryl chlorides, followed by reductive alkylations with Fmoc-protected amino aldehydes are employed to assemble the polyamine backbone. Different acid-stability of the benzhydrylic protective groups allows the selective removal from secondary amines for subsequent branching.

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