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         Ring-closing metathesis (RCM) of dienes is one of the most important methodologies now in use for the assembly of cyclic organic compounds. RCM represents a key step in many synthetic sequences [Chem.Rev.].   Our company can produce Ru-based catalysts such as Grubbs 1st, Grubbs 2nd and and Hoveyda-Grubbs Catalyst..., and can large-scale produce in 2010. We also have developed our own catalysts which are appling for patent. In the same time, we have applied these catalysts in the large scale production of  macrocyclic drugs:

        Take the inhibitor of HCV BILN-2061 for example:

 

         Boehringer-Ingelheim’s 2006 first disclosure of a large-scale RCM approach to the HCV protease inhibitor BILN-2061 provides an interesting case study for those contemplating a large-scale metathesis process. And we can close this macrocyclic at ROOM temperature in DCM.

 

         Large-scale RCM was also used in GlaxoSmithKline’s 2009 synthesis of cathepsin K inhibitor SB-462795:

 

        All of these examples show that it is powerful using RCM in the process of macrocyclic drugs. We are looking forward to cooperating with you!

 

                           All of our APIs products are for research use only. Not for human use. We do not sell to patients.

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