New 6[(2'-dialkylamino)ethyl]-4(3H)-pyrimidinones were prepared by a multistep procedure starting from acetone dicarboxylic acid diethyl ester and urea derivatives. These compounds were used as starting materials to obtain 4-N,N-dialkyl-6-vinyl-pyrimidine derivatives by an unprecedented tandem C-6 side chain Hofmann-like elimination/C-4 pyrimidinone substitution. Among the new derivatives obtained, various compounds show anti-Rubella activity. The inhibition of HIV-1 Reverse Transcriptases (RT), from both wild type and modified viruses, is also reported. (C) 2002 Elsevier Science Ltd. All rights reserved.
A New and Efficient Synthesis of Substituted 6-[(2'-Dialkylamino)ethyl]Pyrimidine and 4-N,N-Dialkyl-6-vinyl-cytosine Derivatives and Evaluation of their Anti-Rubella Activity / Saladino, Raffaele; Ciambecchini, Umberto; Maga, Giovanni; Mastromarino, Paola; Conti, Cinzia; Botta, Maurizio. - In: BIOORGANIC & MEDICINAL CHEMISTRY. - ISSN 0968-0896. - STAMPA. - 10:(2002), pp. 2143-2153. [10.1016/S0968-0896(02)00077-9]
A New and Efficient Synthesis of Substituted 6-[(2'-Dialkylamino)ethyl]Pyrimidine and 4-N,N-Dialkyl-6-vinyl-cytosine Derivatives and Evaluation of their Anti-Rubella Activity
MASTROMARINO, Paola;CONTI, Cinzia;
2002
Abstract
New 6[(2'-dialkylamino)ethyl]-4(3H)-pyrimidinones were prepared by a multistep procedure starting from acetone dicarboxylic acid diethyl ester and urea derivatives. These compounds were used as starting materials to obtain 4-N,N-dialkyl-6-vinyl-pyrimidine derivatives by an unprecedented tandem C-6 side chain Hofmann-like elimination/C-4 pyrimidinone substitution. Among the new derivatives obtained, various compounds show anti-Rubella activity. The inhibition of HIV-1 Reverse Transcriptases (RT), from both wild type and modified viruses, is also reported. (C) 2002 Elsevier Science Ltd. All rights reserved.I documenti in IRIS sono protetti da copyright e tutti i diritti sono riservati, salvo diversa indicazione.
