Acrylamido-quinazolines substituted at the 6-position bind irreversibly to the intracellular ATP binding domain of the epidermal growth factor receptor (EGFR). A general route was developed for preparing 6-substituted-4-anilinoquinazolines from [ 18 F]fluoroanilines for evaluation as EGFR targeting
Synthesis of 6- and 7-propargyloxy derivatives of 4-(3-fluoroanilino)-quinazoline
β Scribed by Helen Trinh Pham; Robert N. Hanson; Sandra L. Olmsted; Anton Kozhushnyan; Adam Visentin; Paul J. Weglinsky; Chris Massero; Kristen Bailey
- Book ID
- 104098657
- Publisher
- Elsevier Science
- Year
- 2011
- Tongue
- French
- Weight
- 393 KB
- Volume
- 52
- Category
- Article
- ISSN
- 0040-4039
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β¦ Synopsis
The preparation of the novel isomeric 6-and 7-propargyloxy derivatives of 4-(3-fluoroanilino)-quinazoline was achieved using a six-step process. An alternate method to the 7-propargyloxy derivative and analogous 7-propargyloxy containing compounds is also described.
π SIMILAR VOLUMES
In the title compound, C 20 H 28 N 4 O 4 Γ3H 2 O, the two morpholine rings adopt chair conformations. The crystal packing is stabilized by intermolecular O-HΓ Γ ΓN and O-HΓ Γ ΓO hydrogen bonds involving the water moleucles.