Selective ther cleavage in the aporphine series. Conversion of (S)-bulbocapnine into (S)-corytuberine and (S)-corydine methyl ether.

Bulbocapnine methyl ether ( 2 ), on treatment with boron halides, affords the aporphine-1,2-diol ( 3 ), the novel aporphines 5 and 6 or the phenanthrene derivative 11 depending on the reaction conditions. 3 can be further transformed into corydine methyl ether ( 4 ); 6 has been converted to corytuberine ( 8 ). Similarly, dehydrobulbocapnine methyl ether 9 was converted to 10 .     

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ASICA Association Internationale pour le Calcul Analogique

     

Catalytic diesel particulate filters reduce the in vitro estrogenic activity of diesel exhaust

An in vitro reporter gene assay based on human breast cancer T47D cells (ER-CALUX) was applied to examine the ability of diesel exhaust to induce or inhibit estrogen receptor (ER)-mediated gene expression. Exhaust from a heavy-duty diesel engine was either treated by iron- or copper/iron-catalyzed diesel particulate filters (DPFs) or studied as unfiltered exhaust. Collected samples included particle-bound and semivolatile constituents of diesel exhaust. Our findings show that all of the samples contained compounds that were able to induce ER-mediated gene expression as well as compounds that suppressed the activity of the endogenous hormone 17beta-estradiol (E2). Estrogenic activity prevailed over antiestrogenic activity. We found an overall ER-mediated activity of 1.63 +/- 0.31 ng E2 CALUX equivalents (E2-CEQs) per m(3) of unfiltered exhaust. In filtered exhaust, we measured 0.74 +/- 0.07 (iron-catalyzed DPF) and 0.55 +/- 0.09 ng E2-CEQ m(-3) (copper/iron-catalyzed DPF), corresponding to reductions in estrogenic activity of 55 and 66%, respectively. Our study demonstrates that both catalytic DPFs lowered the ER-mediated endocrine-disrupting potential of diesel exhaust.     

A Novel Synthesis of Aporphines via 3-Phenylphenethylamines

rac-1,2,10-Trimethoxy-aporphine ( 14 ) and rac-2-ethoxy-10,11-dimethoxyaporphine ( 27 ) have been synthesized from the 3-phenylphenethylamines 9 and 22 by a new route. The 8-phenyl-3,4-dihydroisoquinolines 11 and 24 , the oxo-aporphines 12 and 25 and the rac-nor-aporphines 13 and 26 were obtained as intermediates.     

Biotin synthesis. Preparation of (3aS, 6aR)-1,3-dibenzyl-tetrahydro-4H-thieno(3,4-d)imidazole-2,4(1H)-dione

A modification of the biotin synthesis of Goldberg & Sternbach is described, enantiomers being separated in the first steps and wrong isomers recyclised. The conversion of the lactone 15 to the thiolactone 16 is done by a new method using potassium thioacetate in high boiling solvents.     

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