A n efficient synthesis of the chlorambucil-spermidine conjugate 4 has been achieved via NI,N*-bis-Boc-spermidine and 4 has been shown to crosslink DNA lo4 times more efficiently than chlorambucil itself.

A lead generation and optimization program delivered the highly selective and potent CatC inhibitor 10 as an in vivo tool compound and potential development candidate. Structural studies were undertaken to generate SAR understanding.

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SummaryAromatic compounds bearing an ortho-directing substituent may be deuterated by exchange with deuterium oxide in the presence of a range of cycloocta-1,5-dienyliridium(I)1,3-dionate catalysts. The exchange takes place in several dipolar aprotic solvents and is directly applicable to the deuteration of polar compounds. Isotope incorporation is efficient and regiospecific. The method is applicable to a wide range of ortho-directing groups some of which are only weak directors for alternative ortho-labelling approaches. In addition, the application of microwaves enables labelling within minutes even with sub-stituents which are poor directors.

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