856898-38-9

Upstream product

• 5794-88-7 5-Bromo-2-aminobenzoic acid 
• 124-63-0 methanesulfonyl chloride 
• 20712-12-3 (2-amino-5-bromophenyl)methanol 
• 452350-33-3 methyl 5-bromo-2-[(methylsulfonyl)amino]benzoate 

Relevant academic research and scientific papers

One-pot synthesis of 2-hydroxymethylindoles: via photoredox-catalyzed ketyl-ynamide coupling/1,3-allylic alcohol transposition

An efficient visible-light-mediated ketyl-ynamide coupling by employing ynamides bearing alkyl sulfonyl substituents to deliver eneindolin-3-ols has been developed. Subsequent 1,3-transposition of allylic alcohols in one pot is capable of synthesizing 2-hydroxymethylindoles in generally moderate to good yields. The synthetic utility of this protocol has also been demonstrated by the facile and practical synthesis of two bioactive molecules. The use of readily available substrates, a simple procedure and benign reaction conditions render this method a viable alternative for the synthesis of 2-hydroxymethylindoles. This journal is

NHC-Catalyzed Chemoselective Reactions of Enals and Aminobenzaldehydes for Access to Chiral Dihydroquinolines

An N-heterocyclic carbene (NHC)-catalyzed reaction between α-bromoenals and 2-aminoaldehydes has been developed. Key steps include chemoselective reaction of the NHC catalyst with one of the aldehyde substrates (the bromoenal) to eventually generate an α,β-unsaturated acylazolium intermediate. Addition of the nitrogen atom of aminoaldehyde to the unsaturated azolium ester intermediate followed by intramolecular aldol reaction, β-lactone formation, and decarboxylation leads to chiral dihydroquinolines with high optical purity. The dihydroquinoline products, which are quickly prepared by using this method, can be readily transformed into a diverse set of functional molecules such as pyridines and chiral piperidines.

Compounds, Compositions and Methods

Compounds useful for treating cellular proliferative diseases and disorders by modulating the activity of KSP are disclosed.