291773-89-2

Upstream product

• 1619-62-1 2,2-dimethylmalonic acid diethyl ester 
• 555-96-4 Benzylhydrazine 
• 20570-96-1 benzylhydrazine dihydrochloride 

Downstream Products

• 291773-99-4 1-butyl-4,4-dimethylpyrazolidine-3,5-dione 
• 291774-23-7 2-[[2'-(aminosulfonyl)(1,1'-biphenyl)-4-yl]methyl]-1-butyl-4,4-dimethylpyrazolidine-3,5-dione 

Relevant academic research and scientific papers

Synthesis and pharmacological evaluation of new pyrazolidine-3,5-diones as AT1 angiotensin II receptor antagonists

On the basis of the structure of the non-peptide receptor antagonist irbesartan, a new series of AT1 ligands was designed. In these compounds the central imidazolone nucleus of irbesartan was replaced by a pyrazolidine-3,5-dione structure. The key intermediate N-alkylpyrazolidine-3,5-diones were synthesized according to a new and general method. The most active compounds possess a spirocyclopentane ring at position 4, a linear butyl chain at position 1, and the [2'(5-tetrazolyl)biphenyl-4- yl]methyl or [2'-(benzoylaminosulfonyl)biphenyl-4-yl]methyl group at position 2. Affinity toward the AT1 and AT2 receptors was assessed by the ability of the compounds to competitively displace [3H]AII from its specific binding sites. The most active compounds, 28 and 48, displayed high affinity for the AT1 receptor, good selectivity AT1 versus AT2, and potent in vitro antagonist activity.

A new synthesis of N-alkyl pyrazolidine-3,5-diones and tetrahydropyridazine-3,6-diones

N-alkyl pyrazolidine-3,5-diones and tetrahydropyridazine-3,6-diones have been synthesized by a new method in a three-step sequence from dialkyl malonates or succinates respectively.