Preparation of N-alkylated 5-oxo-3-carboxamyl-1,4-thiazinanes on solid support

Reza Mortezaei, Satoru Ida
Affymax Research Institute, 3410 Central Expressway, Santa Clara, CA 95051, U.S.A.

David A. Campbell
Bayer Pharmaceuticals, 400 Morgan Lane, West Haven, CT 06516-4175, U.S.A.

Abstract
A general method was developed to generate six-membered cyclic thiazinanes on solid support. Three diversity sites were introduced into this scaffold using primary amines, aldehydes, and 2-bromoalkanoic acids. The methodology to prepare individual cyclic thiazinanes as well as combinatorial libraries of these compounds is described.

Keywords
combinatorial library, LC/MS, scaffold, solid support synthesis, 1, 4-thiazinanes