882532-24-3

Upstream product

• 67-56-1 methanol 
• 882531-54-6 C₁₆H₁₂ClFN₂O₂ 
• 882531-54-6 5-(2-Chlorophenyl)-1,3-dihydro-7-fluoro-8-methoxy-2H-1,4-benzodiazepine-2-one 
• 1420683-72-2 2-[(2-chlorophenyl)(imino)methyl]-4-fluoro-5-methoxyphenylamine 
• 873-32-5 2-Chlorobenzonitrile 
• 1420683-69-7 2-[(2-chlorophenyl)iminomethyl]-4,5-difluorophenylamine 
• 3863-11-4 3,4-difluoroaniline 
• 124-41-4 sodium methylate 

Downstream Products

• 882531-87-5 R₁₅₃₀ 
• 1178859-08-9 C₂₁H₂₁ClFN₃O₂ 

Relevant academic research and scientific papers

Discovery of a highly potent, orally active mitosis/angiogenesis inhibitor R1530 for the treatment of solid tumors

A new series of 7,8-disubstituted pyrazolobenzodiazepines based on the lead compound 1 have been synthesized and evaluated for their effects on mitosis and angiogenesis. Described herein is the design, synthesis, SAR, and antitumor activity of these compo

Process for preparing pyrazole functionalized benzodiazepinones

The present invention provides innovative strategies for synthesizing pyrazole ring-functionalized benzodiazepinones. Alternative intermediates and high conversion strategies for forming alpha-aminobenzophenone intermediates involve a combination of aromatic acylation, displacement of electronegative leaving groups with amine, and then N-displacement strategies to produce the desired alpha-aminobenzophenone with primary amine functionality. Reaction strategies are then provided for converting alpha-aminobenzophenones to alpha-aminoamidobenzophenone intermediates with high yield and convenient reaction strategies. These alpha-aminoamidobenzophenone intermediates are then converted into benzodiazepinones. These benzodiazepinones are then converted to pyrazole ring functionalized benzodiazepinones through a series of innovative intermediates and/or reaction strategies.

7,8-Disubstituted pyrazolobenzodiazepines

The present invention provides compounds of formula I wherein R1, R2, R3, R4, and R5 are described herein. The invention also provides syntheses for preparation of such compounds and pharmaceutical compositions containing them. The invention further provides methods for inhibiting kinases, in particular CDK2, for inhibiting angiogenesis, and for treating cancers, in particular breast, colon, prostate, and lung cancer.