Combined Solid Phase and Solution Synthesis of the Fully Protected Segment 74-99 of HIV 1-Protease with the Application of a New Trityl-Linker

Abstract
A new trityl-linker for the strategy of combined solid phase and solution synthesis has been used for the synthesis of the fully protected segment 74-99 of HIV 1-protease. The fully protected fragments 74-81, 82-99 and 90-99 have been synthesized on the polystyrenepolyethylenglykol resin TentaGel, split off with dilute acetic acid and assembled in solution without loss of side-chain protecting groups. After protection of the C-terminus of the fragment 90-99, the second fragment was coupled with TBTU/NMM. The couplings were monitored by IS-MS and HPLC. Racemization was checked by chiral gas-chromatography on a Chirasil-Val capillary.

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