77053-52-2

Upstream product

• 23786-13-2 methyl p-tolylacetate 
• 622-47-9 4-tolylacetic acid 
• 67-56-1 methanol 
• 35675-44-6 4-methylphenylacetyl chloride 
• 25297-16-9 2-bromo-2-(p-tolyl)acetic acid 

Downstream Products

• 66504-76-5 (1R,2S)-1-p-Tolyl-cyclopropane-1,2-dicarboxylic acid dimethyl ester 
• 71195-57-8 bicifadine 
• 86215-53-4 3-methyl-1-(4-methylphenyl)-3-azabicyclo<3.1.0>hexane 
• 86215-31-8 3-Allyl-1-(p-tolyl)-3-azabicyclo<3.1.0>hexan 
• 86215-19-2 3-Cyclopropylmethyl-1-(p-tolyl)-3-azabicyclo<3.1.0>hexan 
• 66504-87-8 (+/-)-1-(4-methylphenyl)-3-azabicyclo[3.1.0]hexan-2,4-dione 
• 83213-67-6 (-)-bicifadine 
• 83213-66-5 (1R,5S)-1-(4-methylphenyl)-3-azabicyclo[3.1.0]hexane 
• 66504-77-6 (1S,5R)-1-p-Tolyl-3-aza-bicyclo[3.1.0]hexane-2,4-dione 
• 66504-84-5 (1R,5S)-1-p-Tolyl-3-aza-bicyclo[3.1.0]hexane-2,4-dione 
• 66504-85-6 (1S,2R)-(-)-1-(4-methylphenyl)-1,2-cyclopropanedicarboxylic acid 
• 66504-83-4 (1R,2S)-(+)-1-(4-methylphenyl)-1,2-cyclopropanedicarboxylic acid 
• 66504-83-4 (1R,2S)-1-p-Tolyl-cyclopropane-1,2-dicarboxylic acid 
• 343946-43-0 1-(p-tolyl)-3-azabicyclo[3.1.0]-hexan-2-one 

Relevant academic research and scientific papers

Diastereo- And Enantioselective Synthesis of Quaternary α-Amino Acid Precursors by Copper-Catalyzed Propargylation

A diastereo- and enantioselective propargylic substitution reaction between propargylic carbonates and α-substituted nitroacetates catalyzed by a Cu-pybox complex is described. This method allows the preparation of a series of non-proteinogenic quaternary α-amino acid precursors featuring two contiguous stereogenic centers and a terminal alkyne moiety in high yields with good to excellent diastereo- and enantioselectivities in most cases. The propargylated adducts were elaborated into a diverse set of quaternary α-amino acid derivatives.

SUBSTITUTED PIPERAZINES AND PIPERIDINES AS MODULATORS OF THE NEUROPEPTIDE Y2 RECEPTOR

The invention provides novel non-peptidic NPY Y2 receptor inhibitors useful in treating or preventing: anxiolytic disorders or depression; injured mammalian nerve tissue; conditions responsive to treatment through administration of a neurotrophic factor; neurological disorders; bone loss; substance related disorders; sleep/wake disorders; cardiovascular disease; obesity; or an obesity-related disorder. Compounds of the invention are also useful in modulating endocrine functions, particularly endocrine functions controlled by the pituitary and hypothalamic glands, and are therefore useful in the treatment or prevention of inovulation and infertility.

ANGIOTENSIN II ANTAGONISTS INCORPORATING A SUBSTITUTED PYRIDOIMIDAZOLYL RING

Substituted heterocycles attached through a methylene bridge to novel substituted phenyl derivatives of the Formula I are useful as angiotensin II antagonists. STR1

1-Aryl-3-azabicyclohexanes, a New Series of Nonnarcotic Analgesic Agents

A series of 1-aryl-3-azabicyclohexanes was synthesized by hydride reduction of 1-arylcyclopropanedicarboximides.Hydroxyphenyl analogues 20, 22, and 24 were prepared by EtSNa-DMF ether cleavage of the corresponding methoxyphenyl analogues 2m, 2n, and 23, respectively, with the secondary amines 20 and 22 going through the N-formyl intermediates 19 and 21.The p-ethoxy analogue 26 was obtained by O-ethylation of 19, followed by base hydrolysis of the amide 25.The greatest analgesic potency in mouse writhing and rat paw-pain assays was observed for para-substituted compounds.Bicifadine, 1-(4-methylphenyl)-3-azabicyclohexane (2b), was the most potent member of the series and is presently undergoing clinical trials in man.Analgesic activity of 2b is limited to the (+) enantiomer 2v, which has the 1R,5S absolute configuration as determined by single-crystal X-ray analysis.The N-methyl analogue (27d) of 2b showed significant analgesic potency, whereas the N-allyl (27a), N-(cyclopropylmethyl) (27b), and N-(n-hexyl) (27c) analogues were inactive.Bicifadine (2b) showed a nonnarcotic profile different from analogous azabicycloalkane and 3-phenylpyrrolidine analgesics.