Beilstein J. Org. Chem.2013,9, 503–509, doi:10.3762/bjoc.9.54
yields and high purity, which is the core moiety of RSV inhibitors.
Keywords: benzothiadiazine-3-one 1,1-dioxide; 3-ethoxy-1,2,4-benzothiadiazine1,1-dioxide; intramolecular aza-Wittig reaction; sultam; Introduction
Sultams have gained popularity in the scientific community especially among synthetic
reaction with 10b at room temperature. In the presence of heat the iminophosphorane intermediate I leads to the formation of the product 3-ethoxy-1,2,4-benzothiadiazine1,1-dioxide 13 (Scheme 3). However, in all other cases we did not carry out the reactions at room temperature for isolation of the
-one 1,1-dioxide can further be alkylated at the 4-position, following a literature procedure, to give the bioactive RSV inhibitors.
Biologically active 1,2,4-benzothiadiazine 1,1-dioxide derivatives.
Retrosynthesis analysis of RSV inhibitors.
Preparation of 3-ethoxy-1,2,4-benzothiadiazine1,1-dioxide
PDF
Graphical Abstract
Figure 1:
Biologically active 1,2,4-benzothiadiazine 1,1-dioxide derivatives.