147149-89-1Relevant articles and documents
A large scale process for the preparation of thymitaq
Malmgren, Hakan,Baeckstroem, Birthe,Solver, Ellen,Wennerberg, Johan
, p. 1195 - 1200 (2008)
The large scale manufacturing of the anticancer agent 2-amino6-methyl-5- (pyridin-4-ylsulfanyl)-3H-quinazolin-4-one dihydrochloride (thymitaq) from 6-bromo-5-methylanthranilic acid is described. The chemical route consists of two chemical steps: formation of a bromoquinazolinone and a copper-mediated Ullman-like coupling between 4-mercaptopyridine and the bromoquinazolinone. During process development, sodium hydride was replaced with sodium hydroxide and a method for removal of copper, based on 2,4,6-trimercapto-s-triazine, was developed. A number of purification operations were performed to ensure a product of pharmaceutical quality.
New straightforward synthesis of 2-amino-6-methyl-5-(pyridin-4-ylsulfanyl)- 3H-quinazolin-4-one
Chen, Wei-Min,Wan, Shan-He
, p. 53 - 61 (2007/10/03)
The synthesis of 2-amino-6-methyl-5-(pyridin-4-ylsulfanyl)-3H-quinazolin-4- one (1) was studied via three different synthetic routes starting from 4-bromo-5-methylisatin. The best route was established, which is a straightforward route via 2-guanidino-5-b