An ortho-lithiation process for the synthesis of...

Details An ortho-lithiation process for the synthesis of... An ortho-lithiation process for the synthesis of...

C - Chemistry, Metallurgy

07

D

C07D 257/04 (2006.01) C07F 1/02 (2006.01) C07F 7/10 (2006.01) C07F 7/22 (2006.01)

Patent

CA 2041620

A process utilizes the tetrazole functional group to direct lithiation at the ortho position of a phenyltetrazole and generate a nucleophilic aryllithium species which then undergoes reaction with an electrophile to generate a 2-substituted 1-(tetrazol-5-yl)benzene. The process is useful in the production of intermediates in the synthesis of angiotensin II antagonists. This novel process is a more cost effective and versatile route for the large-scale preparation of these key intermediates.

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