56965-16-3

Upstream product

• 107182-29-6 2-ethoxy-3,3-dimethyl-2-phenylaziridine 
• 65-85-0 benzoic acid 
• 97422-15-6 2-(3,3-dimethyl-2-phenyl)aziridinyl-β-hydroxyethyl sulfide 
• 97422-18-9 (3,3-dimethyl-3-phenylaziridinyl-2)-2-dimethylaminoethylsulfide 
• 94744-50-0 N-[(9H-fluoren-9-ylmethoxy)carbonyl]-α-aminoisobutyric acid 
• 18903-69-0 2-amino-2-methyl-1-phenylpropan-1-one 
• 98-88-4 benzoyl chloride 
• 6946-08-3 2-amino-2-methyl-1-phenylpropan-1-one hydrochloride salt 
• 1260435-42-4 5-fluoro-4,4-dimethyl-2,5-diphenyl-4,5-dihydrooxazole 

Downstream Products

• 1260435-42-4 5-fluoro-4,4-dimethyl-2,5-diphenyl-4,5-dihydrooxazole 
• 1260435-51-5 N-(2-methyl-1-oxo-1-phenylpropan-2-yl)benzothioamide 
• 1260435-52-6 5-fluoro-4,4-dimethyl-2,5-diphenyl-4,5-dihydrothiazole 
• 1260435-53-7 5-fluoro-4,4-dimethyl-2,5-diphenyl-4,5-dihydrothiazole 
• 1260435-56-0 2,5,5-trimethyl-3,6-diphenyl-2,5-dihydro-1,2,4-triazine 
• 210898-28-5 5,5-dimethyl-3,6-diphenyl-5,6-dihydro-4H-1,2,4-oxadiazin-6-ol 
• 1260435-59-3 5-ethoxy-4,4-dimethyl-2,5-diphenyl-4,5-dihydrooxazole 

Relevant academic research and scientific papers

DAST-mediated cyclization of α,α-disubstituted-α- acylaminoketones: Efficient and divergent synthesis of unprecedented heterocycles

The design of a new potent nonsteroidal ecdysone agonist led to the discovery of a diethylaminosulfur trifluoride (DAST)-mediated cyclization of α,α-disubstituted-α-acylaminoketones. The resulting fluorooxazolines can be ring-opened or selectively substit

Ketone ligands for modulating the expression of exogenous genes via an ecdysone receptor complex

This invention relates to a method to modulate exogenous gene expression in which an ecdysone receptor complex comprising: a DNA binding domain; a ligand binding domain; a transactivation domain; and a ligand is contacted with a DNA construct comprising:

Synthesis and SAR of α-acylaminoketone ligands for control of gene expression

A lead discovery library and a follow-up focused library of α-acylaminoketones were designed based on known dibenzoylhydrazine ecdysone agonists, including GS-E. The compounds were assayed in mammalian cells expressing the ecdysone receptor from Bombyx mori for their ability to cause expression of a reporter gene downstream of an ecdysone response element. The most potent α-acylaminoketones were comparable to GS-E in this assay.

Solid phase synthesis of α-acylamino-α,α-disubstituted ketones

α-Acylamino-α,α-disubstituted ketones are of interest as ecdysone agonists. Solid phase synthesis of prototypical α-acylamino-α,α-disubstituted ketones on two different solid supports is described. In both cases the ketone was formed by reaction of a Grignard reagent with an N-acyl-α,α-disubstituted amino acid immobilized through its carboxylate as a Weinreb amide derivative.

REACTIONS OF AZIRINES WITH SULFUR NUCLEOPHILES. 4. TREATMENT OF 2H-AZIRINE WITH MERCAPTOSUBSTITUTED ACIDS. REACTIONS OF AZIRIDINYL ALKYL SULFIDES WITH CARBOXYLIC ACIDS AND ACYL CHLORIDE DERIVATIVES

Treatment of 2H-azirines with mercaptosubstituted acids and their derivatives leads to β-ketoamides and 2-aziridinyl alkyl sulfides, respectively. 2-Aziridinyl alkyl sulfides, in turn, react with carboxylic acids to give β-ketoamides and substituted ethanethiol derivatives.Acylation of 2-aziridinyl alkyl sulfides with acyl halides generates a variety of products, depending on the reaction conditions; either products derived from cleavage and isomerization of the aziridinyl ring or (1-acylaziridinyl-2) alkyl sulfides are obtained.