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Dicarboxylates of 3-Methylidene-β-lactams: Addition Reactions to the Exocyclic Double Bond, Formation of Spiro-β-lactams, and Reductive Ring Opening by Hydrazines

✍ Scribed by Susanne Gürtler; Michael Johner; Sabine Ruf; Hans-Hartwig Otto


Publisher
John Wiley and Sons
Year
1993
Tongue
German
Weight
790 KB
Volume
76
Category
Article
ISSN
0018-019X

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✦ Synopsis


Dedicated to Prof. Dr. Dr. h.c. mult. Horst Bohme, Marburg, on the occasion of his 85th birthday (1 6.V11.93) 0-, S-, and N-Nucleophiles are added to the exocyclic double bond of the title compounds 1. The addition of 0-or S-nucleophiles yields stable products (Scheme I ) , while addition of N-nucleophiles results in thermally labile compounds (Scheme 2). The reaction is studied by spectroscopic methods. From hydrazine adducts, a spiro[azetidine-3,3'-pyrazolidine] 7 is obtained, and the addition products of methyl-and benzylhydrazine rearrange to pyrazo~-4-cdrboxylates 6. Furthermore, the exocyclic double bond is used for the formation of spiro-p-lactams either by cyclopropane formation or by Diels-Alder reactions (Scheme 4 ) . The steric course of all reactions is studied, and it is shown that all reactions with the double bond occur from the side opposite to the bulkier substituent at C(4) of the p-lactam ring.