Synthesis of variolin B

被引:21
作者
Ahaidar, A
Fernández, D
Pérez, O
Danelón, G
Cuevas, C
Manzanares, I
Albericio, F
Joule, JA
Alvarez, M
机构
[1] Univ Barcelona, Biomed Res Inst, E-08028 Barcelona, Spain
[2] Univ Barcelona, Fac Pharm, Organ Chem Lab, E-08028 Barcelona, Spain
[3] Pharma Mar, Madrid 28770, Spain
[4] Univ Barcelona, Dept Organ Chem, E-08028 Barcelona, Spain
[5] Univ Manchester, Dept Chem, Manchester M13 9PL, Lancs, England
关键词
D O I
10.1016/S0040-4039(03)01551-X
中图分类号
O62 [有机化学];
学科分类号
070303 ; 081704 ;
摘要
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. (C) 2003 Elsevier Ltd. All rights reserved.
引用
收藏
页码:6191 / 6194
页数:4
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