Process for the preparation of biphenyl containing intermediates

Details Process for the preparation of biphenyl containing intermediates Process for the preparation of biphenyl containing intermediates

1995-06-06

1996-09-17

Dentz, Bernard

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

Organic compounds

Sulfonate esters

558 58, 556442, 552105, 560102, C07C30965, C07C30973, C07C 69767

Patent

active

055570020

ABSTRACT:
The present invention provides an industrially advantageous process for preparing a 2-alkyl-3-(biphenyl-4-yl)methyl-3H-imidazo[4,5-b]pyridine derivative represented by the following formula (II) which is a precursor of an antagonist against an angiotensin II receptor useful as an antihypertensive drug, a biphenyl derivative which is a precursor of the substituent of the pyridine derivative, a process for the preparation thereof, and an intermediate useful for the preparation of the biphenyl derivative: ##STR1## The 2-alkyl-3-(biphenyl-4-yl)methyl-3H-imidazo[4,5-b]pyridine derivative can be prepared in a high yield according to the present invention from a 2-amino-5-halogeno-3-nitropyridine derivative through amidation, N-alkylation and reductive cyclization. The halogen atom introduced at the 5-position as a protective group against nitration can be eliminated simultaneously in the step which is conducted thereafter. Thus, this process is industrially advantageous.
Further, the biphenyl derivative of the present invention is excellent in reactivity and purity of the product, thus being an intermediate suitable for the industrial production.

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