761443-69-0Relevant articles and documents
(R)- N - [5 - (2 - methoxy - 2 - phenyl-acetyl) - 1, 4, 5, 6 - tetrahydro-pyrrolo [3, 4 - c] pyrazole - 3 - yl] - 4 - (4 - methyl piperazine - 1 - yl) benzamide synthesis method
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, (2017/02/17)
The invention belongs to the technical field of medicine and relates to a preparation method for PHA739358(Danusertib), i.e., (R)-N-[5-(2-methoxy-2-phenylacetyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole-3-yl]-4-(4-methyl piperazine-1-yl)benzamide. According to the invention, altogether four reaction routes are designed, simple and easily available glycine is used as a raw material, reactions like addition, esterification, amino protection and cyclization are carried out so as to prepare (R)-N-[5-(2-methoxy-2-phenylacetyl)-1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole-3-yl]-4-(4-methyl piperazine-1-yl)benzamide, yield of the route 1, 2 and 4 is more than 25%, respectively, and yield of the route 3 is more than 20%. The preparation method has the advantages of a few reaction steps, simple and convenient post-treatment operation, little time consumption, high yield and low total cost. Thus, a novel method is provided for preparation of the antitumor drug PHA739358.
Potent and selective aurora inhibitors identified by the expansion of a novel scaffold for protein kinase inhibition
Fancelli, Daniele,Berta, Daniela,Bindi, Simona,Cameron, Alexander,Cappella, Paolo,Carpinelli, Patrizia,Catana, Cornel,Forte, Barbara,Giordano, Patrizia,Giorgini, Maria Laura,Mantegani, Sergio,Marsiglio, Aurelio,Meroni, Maurizio,Moll, Juergen,Pittalà, Valeria,Roletto, Fulvia,Severino, Dino,Soncini, Chiara,Storici, Paola,Tonani, Roberto,Varasi, Mario,Vulpetti, Anna,Vianello, Paola
, p. 3080 - 3084 (2007/10/03)
Potent and selective Aurora kinase inhibitors were identified from the combinatorial expansion of the 1,4,5,6-tetrahydropyrrolo[3,4-c]pyrazole bi-cycle, a novel and versatile scaffold designed to target the ATP pocket of protein kinases. The most potent c