A convenient synthesis of N1-substituted 3,4-dihydropyrimidin-2(1H)-ones by cyclocondensation of alpha-chlorobenzyl isocyanates with ethyl N-alkyl(aryl)-beta-aminocrotonates

作者：Sukach VA; Bol'but **; Sinitsa AD; Vovk MV^*

来源：Synlett, 2006, (3): 375-378.

DOI：10.1055/s-2006-92624

• cyclocondensation
• regioselectivity
• alpha-chloroalkyl isocyanates
• dihydropyrimidones
• beta-aminocrotonic esters

A new convenient approach to the synthesis of N1-substituted 3,4-dihydropyrimidin-2(1H)-ones was developed using the regioselective cyclocondensation of alpha-chlorobenzyl isocyanates with ethyl N-alky](aryl)-beta-aminocrotonates. A number of N1-aryl and N1-alkyl substituted Biginelli compounds difficult to obtain by other methods were prepared with high yields.

• 出版日期2006-2-15