196214-24-1

Upstream product

• 2508-29-4 5-hydroxypentylamine 
• 1694-92-4 2-Nitrobenzenesulfonyl chloride 

Downstream Products

• 1052103-49-7 N-(2-nitrobenzenesulfonyl)-2-piperidinone 
• 196214-28-5 N-{5-[Benzyl-(2-nitro-benzenesulfonyl)-amino]-pentyl}-N-(4-methoxy-benzyl)-2,4-dinitro-benzenesulfonamide 
• 196214-35-4 N-Benzyl-N-{5-[ethyl-(4-methoxy-benzyl)-amino]-pentyl}-2-nitro-benzenesulfonamide 
• 196214-31-0 N-Benzyl-N-[5-(4-methoxy-benzylamino)-pentyl]-2-nitro-benzenesulfonamide 
• 196214-26-3 N-Benzyl-N-(5-hydroxy-pentyl)-2-nitro-benzenesulfonamide 

Relevant academic research and scientific papers

MACROCYCLIC AMIDES ACTING AS PLASMEPSIN INHBITORS FOR THE TREATMENT OF MALARIA

The present invention relates to medicine and in particular to the treatment of malarial infections, more particularly to inhibitors of malarial aspartic proteases - plasmepsins. Even more particularly, the invention relates to macrocyclic amides and pharmaceutical compositions thereof and their use as inhibitors for plasmepsins (Plm).

Synthesis and Structural Elucidation of 1,2-Disubstituted 3-Fluoropiperidines

The work described details the reaction between Selectfluor and a series of 1-carbonyloxy and 1-sulfonyl 2-piperidines in order to generate 3-fluoro-2-methoxypiperidines 3a–f. Their subsequent reaction with allyltrimethylsilane, in the presence of BF3 and TiCl4, is then reported. Studies involving a combination of single-crystal X-ray crystallography and NMR spectroscopy indicate that the allylation process is cis-selective for both carbamate and sulfonamide variants and that optimal levels of diastereoselectivity are obtained using the N-2-nitrobenzene sulfonyl (2-Ns) group. In this manner, the synthesis of a series of 2-allyl 3-fluoro-substituted piperidines (5a, c–f) was achieved. The conversion of both the cis and trans-N-tosyl adducts (5d) into 3-fluorinated analogues of the natural products pelletierine (10) and coniine (11) is subsequently detailed.

2,4-Dinitrobenzenesulfonamides: A simple and practical method for the preparation of a variety of secondary amines and diamines

2,4-Dinitrobenzenesulfonamides, readily prepared from primary amines and 2,4-dinitrobenzenesulfonyl chloride, can be alkylated by the Mitsunobu reaction or by the conventional methods to give N,N-disubstituted sulfonamides in excellent yields. Since 2,4-dinitrobenzenesulfonamides can be removed without deprotecting 2-nitrobenzenesulfonamides, a wide variety of diamines could be prepared by the combined use of these protecting/activating groups.