共 48 条
2,3-disubstituted benzo[b]thiophenes from diarylalkynes via electrophilic addition-cyclization and palladium-catalyzed cross-coupling
被引:19
|作者:
Lamanna, Giuseppe
[1
]
Menichetti, Stefano
[1
]
机构:
[1] Univ Florence, Lab Progettaz Sintesi & Studio Eterocicli Biol At, I-50019 Sesto Fiorentino, FI, Italy
关键词:
benzo[b]thiophenes;
cross-coupling;
electrophilic addition;
electrophilic substitution;
phthalimidesulfenyl chloride;
solid phase synthesis;
DIRECTED THROMBIN INHIBITORS;
ONE-POT SYNTHESIS;
ARYL;
DERIVATIVES;
ANTIESTROGENS;
PRECATALYST;
CHLORIDES;
NHC;
D O I:
10.1002/adsc.200700172
中图分类号:
O69 [应用化学];
学科分类号:
081704 ;
摘要:
Diarylalkynes are readily transformed in 3-chlorobenzo[b]thiophenes in a two-step electrophilic addition-cyclization procedure that runs highly efficiently in solution or in the solid phase. The heteroaromatic carbon-chlorine bond participates in palladium-catalyzed Suzuki-Miyaura or Buchwald-Hartwig cross-couplings to give, in a single step, 2,3-disubstituted derivatives of pharmacological relevance.
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页码:2188 / 2194
页数:7
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