The invention provides quinazoline-7-ether derivatives, particularly 4-anilinyl-6-butenamido-quinazoline-7-ether derivatives that are inhibitors of the receptor protein tyrosine kinases (RTK). The compounds are useful in the treatment of diseases and disorders where RTK activity is implicated such as a hyperproliferative diseases (e.g., cancer). Also provided are methods of preparation of the quinazoline derivatives and methods of use as therapeutic agents alone or in a drug combination.
N-fluorobenzenesulfonimide (NFSI) toward the synthesis of diarylsulfones has been developed. The reaction represents a rare example of sulfonylation reaction using NFSI as an efficient sulfonyl donor and the first example of acid-mediated sulfonylation of unactivated arenes with NFSI via selective cleavage of S–N bonds. This protocol provides a concise approach for the construction of pharmaceutically
A Facile Displacement of Tertiary Nitro Group by Hydrogen with Sodium Hydrogentelluride
作者:Hitomi Suzuki、Koji Takaoka、Atsuhiro Osuka
DOI:10.1246/bcsj.58.1067
日期:1985.3
Sodium hydrogentelluride is a useful reagent for replacement of a class of tertiary nitrogroup by hydrogen.
碲化氢钠是一种用氢取代一类叔硝基的有用试剂。
Direct Sulfonylation of Aromatic Rings with Aryl or Alkyl Sulfonic Acid Using Supported P<sub>2</sub>O<sub>5</sub>/Al<sub>2</sub>O<sub>3</sub>
作者:Abdol. R. Hajipour、Amin Zarei、Leila Khazdooz、Seied A. Pourmousavi、Bi Bi F. Mirjalili、A. E. Ruoho
DOI:10.1080/104265090902796
日期:2005.9.1
Direct sulfonylation of aromatic rings with aryl or alkyl sulfonicacid supported P2O5/Al2O3 (w/w 50%) under heterogeneous conditions in short reaction time and high yields.