Objective
Following to new trends in development of
enhanced fragment libraries and design of sharp-focused sets for specific and challenging
tasks we designed and synthesized series unique intermediates. Two types of
functionalized intermediates have been considered as promising and still rare
on the chemical market:
· Functionalized
diazirines as attractive photolabeled fragments widely used in target
identification studies.
· Amino
Boronic acids as proven potent serine proteases and hydrolases reversible inhibitors.
Series of synthesized new intermediates and
validated modifications with automated
parallel synthesis provide a great opportunity of fast access to
qualitative sharp-focused fragment libraries. The world’s largest collection of
reagents, over 120,000 in stock, give a unique chance to design most diverse fragments sets.
We designed series of fragment
libraries intended to be a useful tool in solving of challenging tasks that
possess both high novelty and drug likeness values. Here are few examples of featured
fragment libraries that can be readily synthesized from available building blocks and validated
synthetic procedures.
· Photolabeled Fragment Library:
Scheme1
· Boronic Acids Fragment Library:
Scheme 2
