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p. 1429-1437
Received: 10 June 2005; in revised form: 6 September 2005 / Accepted: 7 September 2005 / Published: 31 December 2005
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| Download PDF Full-text (179 KB) Abstract: Novel representatives of the important group of biologically active dibenzosuberone derivatives were prepared: 3,7-dibromo-5-(dimethylaminoethyl- oxyimino)-10,11-dihydro-5H-dibenzo[a,d]cyclohepta-1,4-diene (1), 3,7-dibromo-5-(3- dimethylaminopropylidene)-10,11-dihydro-5H-dibenzo[a,d]cycloheptene (2) and 1,7- dibromo-5-(3-dimethylaminopropylidene)-10,11-dihydro-5H-dibenzo-[a,d]-cycloheptene (3). These compounds are potential tricyclic antidepressants (TCAs), which are still the most frequently prescribed antidepressants in many countries.
p. 1438-1445
Received: 5 August 2005; in revised form: 18 October 2005 / Accepted: 20 October 2005 / Published: 31 December 2005
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| Download PDF Full-text (131 KB) Abstract: A novel and straightforward solid-phase synthesis of malondiamides containing a free nitrogen has been developed. These intermediates, which can be directly obtained in good yield and purity, can be further derivatised. This approach can be used for the synthesis of large split-and-mix-libraries.
p. 1446-1457
Received: 30 August 2005; in revised form: 21 October 2005 / Accepted: 15 November 2005 / Published: 31 December 2005
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| Download PDF Full-text (143 KB) Abstract: Aryl free-radicals generated at the C-7 position of ethyl indole-2-carboxylates bearing N-allyl and propargylic groups triggered intramolecular cyclizations to furnish a new class of Duocarmycin analogues, formal ethyl pyrrolo[3,2,1-ij]quinoline-2- carboxylate derivatives, through the less favorable 6-endo-trig cyclization mode.
p. 1458-1461
Received: 12 September 2005 / Accepted: 8 October 2005 / Published: 31 December 2005
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| Download PDF Full-text (36 KB) Abstract: A series of eight alkyl and aryl α-nitro ketones were prepared by the potassium dichromate oxidation of the corresponding nitro alcohols. Short reaction times allowed for the easy isolation of pure nitro ketones that are devoid of starting materials and/or other oxidation side products.
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