Synthesis of tetrazol-1-yl analogs of HMG-COA reductase inhibitor BMS180431 (formerly BMY21950)

A series of tetrazol-1-yl analogs were prepared and compared with the corresponding parent tetrazol-5-yl HMGCO-A reductase inhibitors. The generally weaker enzyme inhibitory activity of 2a may be attributed to the shorter distance between the heterocycle and the backbone of the molecule. The corresponding unsubstituted tetrazole parent compound (2c) becomes the most active in this series.