96056-29-0

Upstream product

• 925-90-6 ethylmagnesium bromide 
• 1571-08-0 methyl 4-formylbenzoate 
• 557-20-0 diethylzinc 
• 97-94-9 triethyl borane 

Downstream Products

• 17745-40-3 methyl p-propanoylbenzoate 
• 872254-92-7 3-{4-[1-(4'-trifluoromethyl-biphenyl-4-yloxy)-propyl]-benzoylamino}-propionic acid methyl ester 
• 872254-91-6 4-[1-(4'-trifluoromethyl-biphenyl-4-yloxy)-propyl]-benzoic acid 

Relevant academic research and scientific papers

Two Stereoinduction Events in One C?H Activation Step: A Route towards Terphenyl Ligands with Two Atropisomeric Axes

Herein we disclose the synthesis of original chiral scaffolds—ortho-orientated terphenyls presenting two atropisomeric Ar–Ar axes. These unusual structures were built up by using the C?H activation approach, and remarkably, both chiral axes were controlled with excellent stereoselectivity in a single transformation. During the reaction, not only does atroposelective functionalization of a biaryl precursor occur to establish one stereogenic axis, but an unprecedented atropo-stereoselective C?H arylation also takes place to generate the second stereogenic element. These enantiomerically pure ortho-terphenyls show an original tridimensional structure and thus constitute a unique foundation for building up a library of enantiomerically pure bidentate ligands, such as the new ligands S/N-Biax and diphosphine BiaxPhos.

Dialkylaluminum N, O -dimethylhydroxylamine complex as a reagent to mask reactive carbonyl groups in situ from nucleophiles

Aluminum complexes of N,O-dimethylhydroxylamine are effective reagents to mask carbonyl groups in situ from nucleophilic addition by organolithiums, Grignard reagents, and borohydrides. The utility of this process by selectively adding nucleophiles into carbonyl groups on a variety of structures as well as distinguishing between carbonyl groups on a sensitive natural product is demonstrated. 1H NMR analysis supports the in situ masking of the more reactive carbonyl group.

Nickel-catalyzed alkylation of aldehydes with trialkylboranes

(Chemical Equation Presented) Nickel-catalyzed alkylation of aldehydes with trialkylboranes proceeds smoothly in the presence of a catalytic amount of 5-allyl-1,2,3,4,5-pentamethyl-1,3-cyclopentadiene or an excess of cesium carbonate to afford the corresponding secondary alcohols.

GLUCAGON RECEPTOR ANTAGONISTS, PREPARATION AND THERAPEUTIC USES

The present invention discloses novel compounds of Formula I, or pharmaceutically acceptable salts thereof, which have glucagon receptor antagonist or inverse agonist activity, as well as methods for preparing such compounds. In another embodiment, the invention discloses pharmaceutical compositions comprising compounds of Formula I as well as methods of using them to treat diabetic and other glucagon related metabolic disorders, and the like.

Towards more chemically robust polymer-supported chiral catalysts for the reactions of aldehydes with dialkylzincs.

N-Methyl-alpha,alpha-diphenyl-L-prolinol derivatives with para-bromo substituents in one or both of the phenyl rings are easily bound to crosslinked polystyrene beads containing phenylboronic acid residues using Suzuki reactions. When the products were used as catalysts for the reactions of aldehydes with diethylzinc in toluene at 20 degrees C, the alcohols were produced in chemical yields >90% and with ees of upto 94%. The better of the two supported catalysts gave ees only 0-9% lower than those obtained with the corresponding soluble catalyst. One of the supported catalysts was recycled successfully nine times.

Synthesis of N-[4-[1-ethyl-2-(2,4-diaminofuro[2,3-d] pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid as an antifolate1

N-[4-[1-Ethyl-2-(2,4-diaminofuro[2,3-d] pyrimidin-5-yl)ethyl]benzoyl]-L-glutamic acid 3 was designed and synthesized to investigate the effect of homologation of a C9-methyl to an ethyl on dihydrofolate reductase (DHFR) inhibition and on antitumor activit