1401067-09-1

Basic information

• Product Name: (2R,3S)-1-benzyl 4-tert-butyl 2,3-bis(3,3,3-trifluoropropyl)succinate
• Synonyms: (2R,3S)-1-benzyl 4-tert-butyl 2,3-bis(3,3,3-trifluoropropyl)succinate
• CAS NO: 1401067-09-1
• Molecular Weight: 456.425
• Mol File: 1401067-09-1.mol

Chemical Properties

• CAS DataBase Reference: (2R,3S)-1-benzyl 4-tert-butyl 2,3-bis(3,3,3-trifluoropropyl)succinate(CAS DataBase Reference)
• NIST Chemistry Reference: (2R,3S)-1-benzyl 4-tert-butyl 2,3-bis(3,3,3-trifluoropropyl)succinate(1401067-09-1)
• EPA Substance Registry System: (2R,3S)-1-benzyl 4-tert-butyl 2,3-bis(3,3,3-trifluoropropyl)succinate(1401067-09-1)

Safety Data

• Hazardous Substances Data: 1401067-09-1(Hazardous Substances Data)

Upstream product

• 100-39-0 benzyl bromide 
• 1401065-46-0 (4S)-4-benzyl-3-(5,5,5-trifluoropentanoyl)-1,3-oxazolidin-2-one 
• 1401067-07-9 tert-butyl (3R)-3-(((4S)-4-benzyl-2-oxo-1,3-oxazolidin-3-yl)carbonyl)-6,6,6-trifluorohexanoate 
• 1401067-03-5 (2R,3S)-3-(tert-butoxycarbonyl)-6,6,6-trifluoro-2-(3,3,3-trifluoropropyl)hexanoic acid 
• 407-62-5 5,5,5-trifluoropentanoic acid 
• 1401067-08-0 (R)-2-(2-(tert-butoxy)-2-oxoethyl)-5,5,5-trifluoropentanoic acid 
• 120097-63-4 3,3,3-trifluoropropyl trifluoromethanesulfonate 

Downstream Products

• 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 
• 1401067-34-2 (2S,3R)-6,6,6-trifluoro-3-((⁽³⁵⁾-1-methyl-2-oxo-5-phenyl-2,3-dihydro-1H-1,4-benzodiazepin-3-yl)carbamoyl)-2-(3,3,3-trifluoropropyl)hexanoic acid 
• 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 
• 1584647-27-7 (2R,3S)-N-((3S)-5-(3-fluorophenyl)-9-methyl-2-oxo-2,3-dihydro-1H-1,4-benzodiazepin-3-yl)-2,3-bis(3,3,3-trifluoropropyl)succinamide 
• 1584648-36-1 (2S,3R)-tert-butyl 6,6,6-trifluoro-3-(((S)-5-(3-fluorophenyl)-9-methyl-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)carbamoyl)-2-(3,3,3-trifluoropropyl)hexanoate 
• 1584648-37-2 (2S,3R)-6,6,6-trifluoro-3-(((S)-5-(3-fluorophenyl)-9-methyl-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)carbamoyl)-2-(3,3,3-trifluoropropyl)hexanoic acid 
• 1584647-28-8 (2R,3S)-N-((3S)-5-(3-chlorophenyl)-9-ethyl-2-oxo-2,3-dihydro-1H-1,4-benzodiazepin-3-yl)-2,3-bis(3,3,3-trifluoropropyl)succinamide 
• 1584648-38-3 (2S,3R)-tert-butyl 3-((5-(3-chlorophenyl)-9-ethyl-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)carbamoyl)-6,6,6-trifluoro-2-(3,3,3-trifluoropropyl)hexanoate 
• 1584647-29-9 (2S,3R)-3-((5-(3-chlorophenyl)-9-ethyl-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)carbamoyl)-6,6,6-trifluoro-2-(3,3,3-trifluoropropyl)hexanoic acid 
• 1584648-45-2 (2S,3R)-tert-butyl 6,6,6-trifluoro-3-((5-(3-fluorophenyl)-9-(hydroxymethyl)-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)carbamoyl)-2-(3,3,3-trifluoropropyl)hexanoate 
• 1584648-46-3 (2S,3R)-6,6,6-trifluoro-3-((5-(3-fluorophenyl)-9-(hydroxymethyl)-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)carbamoyl)-2-(3,3,3-trifluoropropyl)hexanoic acid 
• 1584648-52-1 (S)-((S)-3-((2R,3S)-3-carbamoyl-6,6,6-trifluoro-2-(3,3,3-trifluoropropyl)hexanamido)-5-(3-fluorophenyl)-9-methyl-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-1-yl)methyl 2-((tert-butoxycarbonyl)amino)-3-methylbutanoate 
• 1584648-47-4 (R)-tert-butyl 2-((tert-butoxycarbonyl)amino)-3-(((2S,3R)-6,6,6-trifluoro-3-(((S)-5-(3-fluorophenyl)-9-methyl-2-oxo-2,3-dihydro-1H-benzo[e][1,4]diazepin-3-yl)carbamoyl)-2-(3,3,3-trifluoropropyl)hexanamido)thio)propanoate 
• 1584647-90-4 tert-butyl S-(((2S,3R)-6,6,6-trifluoro-3-(((3S)-5-(3-fluorophenyl)-9-methyl-2-oxo-2,3-dihydro-1H-1,4-benzodiazepin-3-yl)carbamoyl)-2-(3,3,3-trifluoropropyl)hexanoyl)amino)-L-cysteinate 

Relevant articles and documents

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

SUBSTITUTED 1,5-BENZODIAZEPINONE COMPOUNDS

Disclosed are compounds of Formula (I): wherein: R1 is CH2CH2CF3; R2 is CH2CH2CF3, CH2(cyclopropyl), or phenyl; R3 is H or CH3; Ring A is phenyl or pyridinyl; and Rx, Ry, Ra, Rb, y, and z are defined herein. 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.

N-SUBSTITUTED BIS(FLUOROALKYL)-1,4-BENZODIAZEPINONE COMPOUNDS AS NOTCH INHIBITORS

Disclosed are compounds of Formula (I): wherein: R1 is -CH2CH2CF3; R2 is -CH2CH2CF3, or -CH2CH2CH2CF3; R3 is -CH

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.

BIS(FLUOROALKYL)-1,4-BENZODIAZEPINONE COMPOUNDS AND PRODRUGS THEREOF

Disclosed are compounds of Formula (I) and/or salts thereof: wherein R1 is —CH2CH2CF3; R2 is —CH2CH2CF3 or —CH2CH2CH2CF3; R3 is H, —CH3, or Rx; R4 is H or Ry; Ring A is phenyl or pyridinyl; and Rx, Ry, Ra, Rb, y, and z are defined herein. 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; or as prodrugs of such compounds.

TRICYCLIC HETEROCYCLIC COMPOUNDS AS NOTCH INHIBITORS

Disclosed are compounds of Formula (I), wherein: X is O or -NR3; R1 is -CH2CH2CH3, -CH2CF3, -CH2CH2CF3, -CH2CF2CH3, -CH2CH2CH2CF3, -CH2CH2CF2CH3, -CH2CH(CH3)CF3, -CH2CH2CH2F, or CH2(cyclopropyl); R2 is -CH2CH2CH3, -CH2CF3, -CH2CH2CF3, -CH2CF2CH3, -CH2CH2CH2CF3, -CH2CH2CH2F, -CH2CH(CH3)CF3, CH2CH2CF2CH3, -CH2(cyclopropyl), -CH(CH3)(cyclopropyl), phenyl, fluorophenyl, chlorophenyl, trifluorophenyl, methylisoxazolyl, pyridinyl, formula (i), formula (ii), formula (iii), formula (iv) or formula (v); Ring A is phenyl or pyridinyl; and R3, Ra, Rb, Rc, y, and z are defined herein. 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.

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.