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A One‐Pot, One‐Operation [3+3] Annulation Approach to Benzothiazines
Author(s) -
Harmata Michael,
Pavri Neville
Publication year - 1999
Publication title -
angewandte chemie international edition
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 5.831
H-Index - 550
eISSN - 1521-3773
pISSN - 1433-7851
DOI - 10.1002/(sici)1521-3773(19990816)38:16<2419::aid-anie2419>3.0.co;2-i
Subject(s) - amination , annulation , intramolecular force , condensation , chemistry , palladium , aryl , medicinal chemistry , organic chemistry , combinatorial chemistry , catalysis , physics , alkyl , thermodynamics
Enantiomerically pure 2,1‐benzothiazines are readily prepared by a one‐pot, one‐operation procedure consisting of a palladium‐catalyzed aryl amination of an ortho ‐bromobenzaldehyde with a sulfoximine followed by an intramolecular condensation reaction [Eq. (1)]. BINAP=1,1′‐binaphthalene‐2,2′‐diylbis(diphenylphosphane).