Addition of [3-14 C]D/L-tryptophan to the fermentation broth allowed radiofermentative labeling of staurosporine. The approach providing [4c,7a-14 C 2 ]staurosporine in a range from 700 to 1300 MBq/mmol was straightforward and easy to handle as well as safe from a radioprotection point of view. The presented example underlines that close cooperation of microbiologists and radiochemists is a requisite for the success of this approach.

Compound (I) is a potent inhibitor of multidrug resistance-associated proteins with IC50 values four times better than cyclosporin. -(LEYERS, S.; HAECKER, H.-G.; WIENDLOCHA, J.; GUETSCHOW, M.; WIESE*, M.; Bioorg. Med.

tion. -Treatment of anthranilic acids and the amino acid (VI) with CS2 allows mild and easy access to fused thiazine-2,4-dithiones. Subsequent reaction with alkyl halides leads to 2-alkylsulfanyl derivatives like (V) and (VIII). The mechanism is discussed. -(OTTERSBACH, P. A.; ELSINGHORST, P. W.; HAECKER, H.-G.; GUETSCHOW*, M.; Org. Lett. 12 (2010) 16, 3662-3665,

1,2-Dihydro-2-thioxo-4H-3,1-benzothiazin-4-one: Formation from Carbon Disulfide and Isatoic Anhydride. -The reaction affords unexpectedly the benzothiazinone (III) as sole product. It can be readily methylated to give the selective inhibitor (V) of human leukocyte elastase. -(OTTERSBACH, P.; HAECKER, H.-G.; ELSINGHORST, P. W.; SCHNAKENBURG, G.; GUETSCHOW*, M.; Tetrahedron Lett. 51 (