Ortho-lithiation process for the synthesis of 2-substituted 1-(t

Details Ortho-lithiation process for the synthesis of 2-substituted 1-(t Ortho-lithiation process for the synthesis of 2-substituted 1-(t

1990-05-02

1991-08-13

Springer, David B.

Organic compounds -- part of the class 532-570 series

Organic compounds

Heterocyclic carbon compounds containing a hetero ring...

548101, 548110, 548109, C07D25702, C07F 300, C07F 500, C07F 100

Patent

active

050398148

ABSTRACT:
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.

REFERENCES:
patent: 3534113 (1970-10-01), Eastham et al.
patent: 4870186 (1989-09-01), Aldrich et al.

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