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Directed Synthesis of Nonsymmetrical Bis‐Steroidal Pyrazines and the First Biologically Active Cephalostatin Analogues
Author(s) -
Drögemüller Michael,
Jautelat Rolf,
Winterfeldt Ekkehard
Publication year - 1996
Publication title -
angewandte chemie international edition in english
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 0570-0833
DOI - 10.1002/anie.199615721
Subject(s) - chemistry , biological activity , combinatorial chemistry , sequence (biology) , biochemistry , in vitro
Thermolysis of vinylazides affords azirines that can be captured in situ with enamino ketones. This reaction sequence (see below) was developed into a new general method for the preparation of nonsymmetrical pyrazines and applied to the synthesis of cephalostatin analogues with high biological activity.