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Synthesis of variolin B |
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| Authors: | Abderaouf Ahaidar,David Ferná ndezOlga Pé rez,Gerardo Daneló nCarmen Cuevas,Ignacio ManzanaresFernando Albericio,John A. JouleMercedes Á lvarez, |
| Affiliation: | a Biomedical Research Institute, Barcelona Scientific Park, University of Barcelona, Josep Samitier 1-5, E 08028 Barcelona, Spain b Laboratory of Organic Chemistry, Faculty of Pharmacy, University of Barcelona, Avda. Joan XXIII s/n, E 08028 Barcelona, Spain c Pharma Mar, Avda Reyes Católicos 1, 28770 Colmenar Viejo, Madrid, Spain d Department of Organic Chemistry, Universitat de Barcelona, Mart?́ Franqués 1-11, E 08028 Barcelona, Spain e Chemistry Department, The University of Manchester, Manchester M13 9PL, UK |
| Abstract: | The total synthesis of variolin B from 4-methoxy-7-azaindole is described. The preparation of the protected amino derivative 10 and a coupling reaction of the iodo derivative 12 with 2-acetylamino-4-trimethylstannylpyrimidine are the key steps of the sequence. The use of N-tosyldichloromethanimine for the cyclisation step afforded a good entry to the 9-aminopyrido[3′,2′:4,5]pyrrolo[1,2-c]pyrimidine system. Variolin B was obtained from the triply protected tetracyclic compound 13 in two steps. |
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