Communication: polymer-assisted solution-phase synthesis of 4,5-dihydro-1,4-benzoxazepin-3(2H)-ones.
The polymer assisted solution phase (PASP) synthesis of 4,5-dihydro-1,4-benzoxazepin-3(2H)-ones is described. Using salicylic aldehydes, alpha-bromo acetic acid esters, and primary amines as broadly variable building blocks, the target molecules were obtained in a straightforward manner. The use of polymer bound reagents and scavengers greatly simplified workup, and avoided the use of protecting groups. A small library was prepared, showing the feasibility of the synthetic concept for the generation of larger sets of screening compounds.
Carreras
Ignacio
I
Bayer CropScience AG, Alfred-Nobel-Str. 50, D-40789 Monheim, Germany.
Scherkenbeck
Jürgen
J
Paulitz
Christian
C
D001584:Benzoxepins / Q000138:chemical synthesis* / Q000494:pharmacology; D020650:Combinatorial Chemistry Techniques; D011108:Polymers / Q000737:chemistry; D012996:Solutions
D001584:Benzoxepins; D011108:Polymers; D012996:Solutions