16064-08-7

White Solid

6-Iodoquinazolin-4-one is an intermediate in the synthesis of Lapatinib (L175800).

Using 2-amino-5-iodobenzoic acid and trimethyl orthoformate as starting materials, the synthesis procedure of Examples I-2 was followed, but the reaction solvent was replaced from methanol to acetonitrile. Upon completion of the reaction, 6-iodoquinazolin-4-one was obtained by post-processing in a yield of 0.98 g and 94% yield.

[1] Patent: EP1477481, 2004, A1. Location in patent: Page 17
[2] Patent: EP1477481, 2004, A1. Location in patent: Page 16-17
[3] Patent: EP1477481, 2004, A1. Location in patent: Page 17
[4] Patent: EP1477481, 2004, A1. Location in patent: Page 17
[5] Patent: EP1477481, 2004, A1. Location in patent: Page 17