40358-34-7

Upstream product

• 3967-01-9 4-methyl-4,5-dihydro-1H-benzo[b][1,4]diazepin-2(3H)-one 
• 674-82-8 4-methyleneoxetan-2-one 
• 95-54-5 1,2-diamino-benzene 

Downstream Products

• 887757-58-6 2-bromo-5-[(4-methyl-2,3,4,5-tetrahydro-1H-1,5-benzodiazepin-1-yl)carbonyl]phenyl methyl ether 
• 136320-04-2 (9R,12R)-12-(3,4-Dichloro-phenyl)-9-methyl-1,8-diaza-tricyclo[6.3.1.0^2,7]dodeca-2⁽⁷⁾,3,5-triene 
• 136320-06-4 2,4-Dibromo-6-((9R,12R)-9-methyl-1,8-diaza-tricyclo[6.3.1.0^2,7]dodeca-2⁽⁷⁾,3,5-trien-12-yl)-phenol 

Relevant academic research and scientific papers

Ru-Catalyzed Deoxygenative Transfer Hydrogenation of Amides to Amines with Formic Acid/Triethylamine

A ruthenium(II)-catalyzed deoxygenative transfer hydrogenation of amides to amines using HCO2H/NEt3 as the reducing agent is reported for the first time. The catalyst system consisting of [Ru(2-methylallyl)2(COD)], 1,1,1-tris(diphenylphosphinomethyl) ethane (triphos) and Bis(trifluoromethane sulfonimide) (HNTf2) performed well for deoxygenative reduction of various secondary and tertiary amides into the corresponding amines in high yields with excellent selectivities, and exhibits high tolerance toward functional groups including those that are reduction-sensitive. The choice of hydrogen source and acid co-catalyst is critical for catalysis. Mechanistic studies suggest that the reductive amination of the in situ generated alcohol and amine via borrowing hydrogen is the dominant pathway. (Figure presented.).

Metal-free tandem cyclization/hydrosilylation to construct tetrahydroquinoxalines

A one-pot tandem procedure involving cyclization and sequential hydrosilylation of imines and amides under the catalysis of B(C6F5)3 has been developed for the step-economical construction of 1,2,3,4-tetrahydroquinoxalines directly from readily available 1,2-diaminobenzenes, α-ketoesters and low-cost, safe polymethylhydrosiloxane (PMHS). This metal-free approach provides various products in good to excellent yields, and displays a wide range of substrate scope and a high degree of functional group tolerance even to reduction-sensitive moieties. The choice of hydrosilanes is critical to the catalysis, and PMHS has proved to be optimal. Decreasing the amount of PMHS could enable the reaction to stop at the 3,4-dihydroquinoxalin-2(1H)-one stage. The procedure is convenient and scalable, and neither a dried solvent nor an inert atmosphere is required. Moreover, the enantioselective construction of these products was explored, and promising results were achieved.

2,3,4,5-TETRAHYDRO-1H-1,5-BENZODIAZEPINE DERIVATIVE AND MEDICINAL COMPOSITION

The present invention has its object to provide a 2,3,4,5-tetrahydro-1H-1,5-benzodiazepine derivative represented with the Formula (1) , or the pharmaceutically acceptable salt, which is effective as a therapeutic and prophylactic agent for diabetes, diabetic nephropathy, or glomerulosclerosis.

2,3,4,5-TETRAHYDRO-1H-1,5-BENZODIAZEPINE DERIVATIVE AND MEDICINAL COMPOSITION

A 2,3,4,5-tetrahydro-1H-1,5-benzodiazepine derivative represented by the generalformula (1): [Chemical formula 1] (1) or a pharmaceutically acceptable saltthereof. They are useful as a therapeutic/preventive agent for diabetes, diabeticnephropathy, or glomerulosclerosis.

STEREOSELECTIVE BRIDGING OF TETRAHYDRO-1,5-BENZODIAZEPINES

A reaction of tetrahydro-1,5-benzodiazepines with aromatic aldehydes which yields the hitherto unknown 1,5-methanotetrahydro-1,5-benzodiazepines as a single stereoisomer is described.The stereochemistry of the products is established using proton nmr spec