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One‐Pot Directed Alkylation/Deprotection Strategy for the Synthesis of Substituted Pyrrole[3,4‐ d ]pyridazinones
Author(s) -
Nair Reji N.,
Bannister Thomas D.
Publication year - 2015
Publication title -
european journal of organic chemistry
Language(s) - English
Resource type - Journals
SCImago Journal Rank - 0.825
H-Index - 155
eISSN - 1099-0690
pISSN - 1434-193X
DOI - 10.1002/ejoc.201403491
Subject(s) - chemistry , alkylation , pyrrole , combinatorial chemistry , organic chemistry , medicinal chemistry , catalysis
In the course of a structure–activity relationship study of pyrrole[3,4‐ d ]pyridazinones, we optimized conditions for a one‐pot directed lithiation/alkylation reaction that also promoted in situ cleavage of a tert ‐butoxycarbonyl (Boc) protecting group on the pyrrole ring. The efficiency of the process gave access to a number of substituted analogs of interest as possible antitumor agents.