66896-49-9

Upstream product

• 6407-34-7 methyl-1 ethylideneamine 
• 591-51-5 phenyllithium 
• 934-53-2 cumenyl chloride 
• 4747-74-4 α,α-dimethylbenzyl isocyanate 
• 826-55-1 2-methyl-2-phenylpropionic acid 
• 25343-67-3 (1-isothiocyanato-1-methyl-ethyl)-benzene 
• 86972-27-2 methylene-(1-methyl-1-phenyl-ethyl)-amine 

Downstream Products

• 875-30-9 1,3-dimethylindole 
• 98-83-9 isopropenylbenzene 
• 102660-50-4 N-Methyl-N-<2-phenyl-propyl-(2)>-N'-naphthyl-(1)-harnstoff 

Relevant academic research and scientific papers

Palladium(II)-Catalyzed C(sp2)-H Carbonylation of Sterically Hindered Amines with Carbon Monoxide

A palladium-catalyzed, amine-directed C(sp2)-H carbonylation of α,α-disubstituted benzylamine under 1 atm of CO for the facile synthesis of sterically hindered benzolactam has been developed. The key to success is the use of 2,2,6,6-tetramethyl-1-piperidinyloxy as the crucial sole oxidant. The synthetic utility of this transformation has been demonstrated by the first concise synthesis of the natural product spiropachysin-20-one.

A Copper-Catalyzed Aerobic [1,3]-Nitrogen Shift through Nitrogen-Radical 4-exo-trig Cyclization

A novel radical [1,3]-nitrogen shift catalyzed by copper diacetate under an oxygen atmosphere (1 atm) has been developed for the construction of a diverse range of indole derivatives from α,α-disubstituted benzylamine. In this reaction, oxygen was used as a clean terminal oxidant, and water was produced as the only by-product. Five inert bonds were cleaved, and two C?N bonds and one C?C double bond were constructed in one pot during this transformation. This unique method demonstrated broad application protential for the late-stage modification of biologically active natural products and drugs. Mechanistic investigations indicate that a unique 4-exo-trig cyclization of an aminyl radical onto a phenyl ring is involved in the catalytic cycle.

RENIN INHIBITORS

The present invention relates to novel renin inhibitors of the general Formula (I), and their use as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds. These novel renin inhibitors are used in treating cardiovascular events and renal insufficiency.

Synthesis of 5-alkoxy-4-alkylamino-1,2-benzoquinones

A simple and efficient method is described for a general synthesis of 4-dialkylamino-5-methoxy-1,2-benzoquinones 3 which involves, in polar solvents, a regioselective (>95%) nucleophilic monosubstitution by a wide range of secondary aliphatic amines on an easily prepared 1,2-quinone 1. Regioselectivity is not observed in the reaction of primary amines with 1, but a further reaction with an alcohol in basic medium allows valorization of the undesirable product.