Piperazic acid derivatives inhibit Gli1 in Hedgehog signaling pathway
Piperazic acid, a non-proteinogenic amino acid, found in complex secondary metabolites and peptide natural substances, has shown down regulation of Gli1 expression in Hedgehog signaling pathway in cell based assays. Further structure activity relationship
IMPROVED PROCESS FOR THE MANUFACTURE OF 1,2-DISUBSTITUTED HEXAHYDROPYRIDAZINE-3-CARBOXYLIC ACIDS AND ESTERS THEREOF
The invention relates to an improved process for the manufacture of 1,2-disubstituted hexahydro-pyridazine-3-carboxylic acids and esters thereof by reacting N,N’-disubstituted hydrazine with 2,5-dihalogenated valeric acids and thereof by means of phase transfer catalysis. Said pyridazine carboxylic acids and esters thereof can be used as intermediates for the production of pharmaceutical products
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Page/Page column 13-14
(2010/02/11)
Process for preparing hexahydropyridazine-3-carboxylic acid derivatives
According to the process of the invention, the hexahydropyridazine-3-carboxylic acid derivatives are prepared by reacting a compound of formula (II) with a compound of formula (III) in the presence of a base with a pK of greater than or equal to 8.5, in a ketone organic solvent, to obtain an intermediate compound that is not isolated and that is treated with a basic aqueous medium. By means of this process, the derivatives are obtained more quickly and more economically.
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Page 3
(2008/06/13)
PREPARATION OF 1-(BENZYLOXYCARBONYL)HEXAHYDRO-3-PYRIDAZINE CARBOXYLIC ACID, A PROTECTED PIPERAZIC ACID
A preparation of 1-(benzyloxycarbonyl)hexahydro-3-pyridazinecarboxylic acid in five steps (73percent overall yield) from 4-phenylurazole is described.
Adams, C. E.,Aguilar, D.,Hertel, S.,Knight, W. H.,Paterson, J.
p. 2225 - 2232
(2007/10/02)
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