In this communication, we report diastereoselective addition of allyl reagents to N-monoprotected and N,N-diprotected L-alaninals, and the characterization of the products.

(Final version not submitted in time.)

A close structural relationship between - and -santenones, occuring in Indian sandalwood (Santalum album), results in serious difficulties in the preparation of their derivatives in a pure form.1,2

Convenient synthesis of 1.2.5-(1.3.4)-oxadiazolyl-1,2,4-oxadiazoles by reaction between corresponding amidoximes and nitriles in present of ZnCl2 and HCL has been elaborated.

Phosgenated p-nitrophenyl(polystyrene)ketoxime (Phoxime™) resin (1) has been previously utilized as a latent isocyanate equivalent. The Nautilus™ 2400 automated organic synthesizer was used to determine the optimal temperature for thermolysis of the polymer-bound oxime-carbamate derived from Phoxime resin and subsequent amine addition to give a urea in solution.

Commonly, molecules synthesized on a solid support are attached to the solid phase by a linker entity, often an acid labile linker. A commonly used acid labile linker is the "Rink-linker"1 which provides solid phase attachment via an amide or an ester bond. Upon acid treatment target molecules are released, which all bear a "trace of the linker", such as an acid or primary amide functionality. Here, we describe a method to constitute a much wider variety of molecules by trapping a "Rink-cation" with a number of alcohols, amines or thiols.

Solid supports carrying a photolabile linker of the 3'-methoxybenzoin type were prepared by a rapid solid phase synthesis method. Alternatively, the linker was preassembled in solution by a more lengthy procedure and then coupled onto polystyrene via its carboxymethyl handle. `Safety catch' linkers of this type are expected to play an important role for the preparation of combinatorial libraries suitable for a variety of miniaturized screening methods, where `reagentless' release of compounds from the carrier is crucial

Highly reactive, polystyrene-bound thiocarbamoyl chlorides and isothiocyanates have been used as key intermediates in a new, robust solid-phase synthesis of substituted thiophenes.

Herpes Simplex virus type 1 thymidine kinase (HSV1 TK) phosphorylates thymidine (dT) to thymidine monophosphate (dTMP) playing a key role in reactivation from the latency and replication of herpes simplex viruses. Acyclovir (ACV) and gancyclovir (GCV) are today the only therapeutic compounds to interfere with a severe HSV infection. Those molecules act as fraudulent substrates blocking virus proliferation by dead end complexes with the viral DNA after being activated by the HSV-specific TK. Furthermore, HSV1 TK was more recently used as a suicide enzyme in gene therapy of cancer (1,2) and AIDS (3) in combination with ACV. The molecular basis of the selective therapy, that uses HSV1 TK as target, is the difference in substrate specificity between the human cellular and the herpesviral TK isoenzymes. Because of the important therapeutic implications, HSV is not only linked to viral infection but also with other diseases such as Kaposi's Sarcoma (4) and Alzheimer disease (5), and the increase of resistance towards ACV and GCV, intensive efforts have been directed towards the search of new compounds with general antiviral activity (6). In this study we report the results of a first cycle of structure-based drug-design aiming the development of new compounds for antiviral and gene therapy.

Jochen Temper, B. Vogler and W. Kraus