1401067-34-2

Upstream product

• 1186202-35-6 5,5,5-trifluoro-n-valeryl chloride 
• 108895-98-3 benzyl 2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-ylcarbamate 
• 108895-97-2 2-α-(benzyloxycarbonyl)glycinyl)amino>benzophenone 
• 1401067-08-0 (R)-2-(2-(tert-butoxy)-2-oxoethyl)-5,5,5-trifluoropentanoic acid 
• 1401067-07-9 tert-butyl (3R)-3-(((4S)-4-benzyl-2-oxo-1,3-oxazolidin-3-yl)carbonyl)-6,6,6-trifluorohexanoate 
• 1401065-46-0 (4S)-4-benzyl-3-(5,5,5-trifluoropentanoyl)-1,3-oxazolidin-2-one 
• 1401067-04-6 (2R,3R)-3-(tert-butoxycarbonyl)-6,6,6-trifluoro-2-(3,3,3-trifluoropropyl)hexanoic acid 
• 1401067-00-2 (4S)-4-(propan-2-yl)-3-(5,5,5-trifluoropentanoyl)-1,3-oxazolidin-2-one 
• 407-62-5 5,5,5-trifluoropentanoic acid 
• 1049037-18-4 tert-butyl 5,5,5-trifluoropentanoate 
• 103421-61-0 3-amino-1-methyl-5-phenyl-1,3-dihydro-2H-1,4-benzodiazepin-2-one 
• 1401067-09-1 (2R,3S)-1-benzyl 4-tert-butyl 2,3-bis(3,3,3-trifluoropropyl)succinate 
• 1401067-01-3 tert-butyl (3R)-6,6,6-trifluoro-3-(((4S)-4-isopropyl-2-oxo-1,3-oxazolidin-3-yl)carbonyl)-2-(3,3,3-trifluoropropyl)hexanoate 
• 1401067-05-7 tert-butyl (2S,3R)-6,6,6-trifluoro-3-(((3S)-1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl)carbamoyl)-2-(3,3,3-trifluoropropyl)hexanoate 

Downstream Products

• 1401066-79-2 (2R,3S)-N-((3S)-1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl)-2,3-bis(3,3,3- trifluoropropyl)succinamide 
• 1581704-49-5 (2S,3R)-N-((4-(dimethylamino)-1-piperidinyl)methyl)-N’-((3S)-1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl)-2,3-bis(3,3,3-trifluoropropyl)succinamide 
• 1581704-50-8 (2S,3R)-N-((4-hydroxy-1-piperidinyl)methyl)-N’-((3S)-1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl)-2,3-bis(3,3,3-trifluoropropyl)succinamide 
• 1581704-51-9 (2S,3R)-N-((3-hydroxy-1-pyrrolidinyl)methyl)-N’-((3S)-1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl)-2,3-bis(3,3,3-trifluoropropyl)succinamide 
• 1581704-52-0 C₃₃H₄₀F₆N₆O₃ 
• 1581704-53-1 (2R,3S)-N-((3S)-1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl)-N’(1-pyrrolidinylmethyl)-2,3-bis(3,3,3-trifluoropropyl)succinamide 
• 1581704-41-7 (2S,3R)-N-((isobutylamino)methyl)-N’-((3S)-1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl)-2,3-bis(3,3,3-trifluoropropyl)succinamide 
• 1581704-66-6 tert-butyl 2-((2S,3R)-6,6,6-trifluoro-3-((S,Z)-1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-ylcarbamoyl)-2-(3,3,3-trifluoropropyl)hexanamidothio) ethylcarbamate 
• 1581704-42-8 (2S,3R)-N-((2-Aminoethyl)sulfanyl)-N’-((3S)-1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl)-2,3-bis(3,3,3-trifluoropropyl)succinamide 
• 1581704-43-9 S-(((2S,3R)-6,6,6-trifluoro-3-(((3S)-1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl)carbamoyl)-2-(3,3,3-trifluoropropyl)hexanoyl)amino)-L-cysteine 
• 1581704-44-0 (2S,3R)-N-((2-(Dimethylamino)ethyl)sulfanyl)-N’-((3S)-1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl)-2,3-bis(3,3,3-trifluoropropyl)succinamide 
• 1581704-45-1 methyl S-(((2S,3R)-6,6,6-trifluoro-3-(((3S)-1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl)carbamoyl)-2-(3,3,3-trifluoropropyl)hexanoyl)amino)-L cysteinate 
• 1581704-46-2 (2R,3S)-N-((3S)-1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl)-N’((4-methyl-1-piperazinyl)methyl)-2,3-bis(3,3,3-trifluoropropyl)succinamide 
• 1581704-47-3 (2R,3S)-N-((3S)-1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl)-N’(1-piperidinylmethyl)-2,3-bis(3,3,3-trifluoropropyl)succinamide 

Relevant academic research and scientific papers

A Practical Approach for Enantio- and Diastereocontrol in the Synthesis of 2,3-Disubstituted Succinic Acid Esters: Synthesis of the pan-Notch Inhibitor BMS-906024

An oxidative intermolecular enolate heterocoupling reaction was employed for the synthesis of anti-2,3-disubstituted succinic acid mono- and differentially protected diesters. Tactical approaches to access all the diastereomers are discussed. The method w

Discovery of clinical candidate BMS-906024: A potent pan-notch inhibitor for the treatment of leukemia and solid tumors

Structure-activity relationships in a series of (2-oxo-1,4-benzodiazepin-3-yl)-succinamides identified highly potent inhibitors of γ-secretase mediated signaling of Notch1/2/3/4 receptors. On the basis of its robust in vivo efficacy at tolerated doses in

PRODRUGS OF 1,4-BENZODIAZEPINONE COMPOUNDS

Disclosed are compounds of Formula (I) and salts thereof, wherein: a) R1 is H or CH3, and R2 is Ry; or b) R1 is Rx and R2 is H; wherein Rx and Ry are disclosed herein.

BISFLUOROALKYL-1,4-BENZODIAZEPINONE COMPOUNDS

Disclosed are compounds of Formula (I) or prodrugs thereof; wherein: R1 is —CH2CF3 or —CH2CH2CF3; R2 is —CH2CF3, —CH2CH2CF3, or —CH2CH2CH2CF3; R3 is H or —CH3; each Ra is independently F, Cl, —CN, —OCH3, and/or —NHCH2CH2OCH3; and z is zero, 1, or 2. Also disclosed are methods of using such compounds to inhibit the Notch receptor, and pharmaceutical compositions comprising such compounds. These compounds are useful in treating, preventing, or slowing the progression of diseases or disorders in a variety of therapeutic areas, such as cancer.