HCID 66707370, compound → HCID 66707309, compound

Participants

Reaction Steps

The following examples can be prepared in analogous fashion to example 1.1, employing in the reduction step [5-methyl-1-(4-nitro-benzyl)-1H-pyrazol-4-yl]-acetic acid tert-butyl ester or in the case of example 2.59 [5-ethyl-1-(4-nitro-benzyl)-1H-pyrazol-4-yl]-acetic acid tert-butyl ester (preparation according to WO2008/138876) instead of [3,5-dimethyl-1-(nitrobenzyl)-1H-pyrazol-4-yl-acetic acid methyl ester and employing in the amide coupling the corresponding carboxylic acids as coupling partners. Each example except for example 2.59 is a single regioisomer; the required intermediates [1-(4-amino-benzyl)-3-methyl-1H-pyrazol-4-yl]-acetic acid tert-butyl ester and [1-(4-amino-benzyl)-5-methyl-1H-pyrazol-4-yl]-acetic acid tert-butyl ester are obtained in a single reaction and are separable by MPLC.

Provenance & Evidence