4699-82-5

Upstream product

• 259144-38-2 N-(2-benzoyl-4-chlorphenyl)-N'-tert-butoxycarbonyl-alaninamide 

Downstream Products

• 41282-00-2 7-chloro-1,3-dihydro-3-methyl-5-phenyl-2H-1,4-benzodiazepine-2-thione 
• 37115-39-2 8-chloro-1-<(dimethylamino)methyl>-4-methyl-6-phenyl-4H-s-triazolo<4,3-a><1,4>benzodiazepine 

Relevant academic research and scientific papers

Preparation of a New Chiral Stationary Phase Based on Macrocyclic Amide Chiral Selector for the Liquid Chromatographic Chiral Separations

A new chiral stationary phase (CSP) based on macrocyclic amide receptor was prepared starting from (1R,2R)-1,2-diphenylethylenediamine. The new CSP was successfully applied to the resolution of various N-(substituted benzoyl)-α-amino amides with reasonably good separation factors and resolutions (α = 1.75 ~ 2.97 and RS = 2.89 ~ 6.82 for 16 analytes). The new CSP was also applied to the resolution of 3-substituted 1,4-benzodiazepin-2-ones and some diuretic chiral drugs including bendroflumethiazide and methylchlothiazide and metolazone. The resolution results for 3-substituted 1,4-benzodiazepin-2-ones and some diuretic chiral drugs were also reasonably good. Chirality 28:253-258, 2016.

Preparation of chiral 1,4-benzodiazepin-2-one-derivatives by reaction of (s)-α-amino acid chloride hydrochlorides etc.

A process is disclosed for preparing optically active 1,4-diazepine-2-ones by reacting an acid chloride-hydrochloride of an optically active α-amino acid with a substituted o-amino benzophenone, to form an intermediate product and subsequently cyclizing the intermediate product to form the desired 1,4-diazepine-2-one. The process is carried out in inert organic or aqueous-organic solvents. The process eliminates the need for using α-amino acids having bound to the amino group a protective group which must be removed before cyclization.

Intermediates for preparing 1,4-benzodiazepine-2-ones having a carboxylic acid ester or amide group in the 3-position

Intermediates for preparing novel benzodiazepines having the formula SPC1 In which R1 is a hydrogen or halogen atom or a trifluoromethyl, loweralkyl, loweralkoxy, nitro or amino group; R2 is a furyl, a thienyl, cyclohexyl, a loweralkyl group or a phenyl group which may be substituted by a halogen atom or by a trifluoromethyl, nitro, loweralkoxy or loweralkyl group; and R3 is a hydrogen atom or a loweralkyl group; and R4 is lowercarbalkoxy, carbamoyl, N-loweralkylcarbamoyl, N,N-diloweralkylcarbamoyl, N-(diloweralkylaminoalkyl)carbamoyl, a group having the formula --COOCat in which Cat is a cation of an alkali metal or a semication of an alkaline earth metal or COOCat.CatOH, said intermediates being ortho-aminoaryl ketimines having the formula SPC2 Wherein R is hydrogen or EQU1 R1, R2, and R3 are as defined above, R4 is a hydrogen atom, a lowercarbalkoxy, carbamoyl, N-loweralkylcarbamoyl, N,N-diloweralkylcarbamoyl, N-(diloweralkylaminoalkyl)-carbamoyl, alkyl or substituted alkyl group; and R5 is a loweralkyl group.