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Showing posts with label ABEMACICLIB. Show all posts
Showing posts with label ABEMACICLIB. Show all posts

Thursday 1 October 2015

ABEMACICLIB, BEMACICLIB







Scheme:
amide compound S-2 under the action of POCl3 to form chlorine imine intermediate aniline 
compound S-1 to accept the attack to give compound S-3, S-3 under basic conditions, pulling
 protons, after nucleophilic aromatic substitution reaction
 benzimidazole compound S-4, followed by S-4 aryl bromide and B2Pin2 by Pd-catalyzed
 reaction, the aromatic substrate was prepared by alcohol
 grease S-5, and chlorinated pyrimidine compounds followed through palladium catalyzed
 Suzuki reaction S-7 to give the coupling product stand.
Secondary amine compound S-8 and S-9 aldehyde through condensation, reduction to
 give an amine compound S-10, S-10 and then in the Pd-catalyzed, biphenyl type CyJohnPhos (structure see below) as well as large steric 
hindrance ligand As the nitrogen source LiHMDS Preparation of 2-aminopyridine compound S-11.
Obtained after S-11, S-7 and its by Buchwald-Hartwig reaction, to give compound S-12, 
S-12 compound and formed methanesulfonate obtained Abemaciclib (Bemaciclib) 
Reference line: US20100160340 breast cancer drug to Pfizer, Novartis and Eli Lilly's 
new drug represented the three companies Palbociclib, Ribociclib and Abemaciclib. 
About Palbociclib, Ribociclib synthesis have already posted.









Scheme:
amide compound S-2 under the action of POCl3 to form chlorine imine intermediate aniline
compound S-1 to accept the attack to give compound S-3, S-3 under basic conditions,
pulling protons, after nucleophilic aromatic substitution reaction benzimidazole compound S-4,
followed by S-4 aryl bromide and B2Pin2 by Pd-catalyzed reaction, the aromatic substrate was
prepared by alcohol grease S-5, and chlorinated pyrimidine compounds followed through
 palladium catalyzed Suzuki reaction S-7 to give the coupling product stand.

Secondary amine compound S-8 and S-9 aldehyde through condensation, reduction to
 give an amine compound S-10, S-10 and then in the Pd-catalyzed, biphenyl type
CyJohnPhos (structure see below) as well as large steric hindrance ligand As the
 nitrogen source LiHMDS Preparation of 2-aminopyridine compound S-11.

Obtained after S-11, S-7 and its by Buchwald-Hartwig reaction, to give compound S-12,
 S-12 compound and formed methanesulfonate obtained Abemaciclib (Bemaciclib) 
Reference line: US20100160340 breast cancer drug to Pfizer, Novartis and
 Eli Lilly's new drug represented the three companies Palbociclib, Ribociclib and Abemaciclib. 
About Palbociclib, Ribociclib synthesis have already posted.




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