170277-84-6Relevant academic research and scientific papers
Construction of carbo- And heterocycles using radical relay cyclizations initiated by alkoxy radicals
Zhu, Hai,Wickenden, Jason G.,Campbell, Natalie E.,Leung, Joe C. T.,Johnson, Kayli M.,Sammis, Glenn M.
supporting information; experimental part, p. 2019 - 2022 (2009/09/08)
An efficient method for the rapid construction of carbo- and heterocycles has been developed using radical relay cyclizations initiated by alkoxy radicals. Linear substrates were cyclized to form a wide range of cyclopentane, pyrrolidine, tetrahydropyran, and tetrahydrofuran derivatives in excellent yields. This methodology was utilized as a key step in the synthesis of the tetrahydrofuran fragment in (-)-amphidino-lide K.
Cyclization strategies for the synthesis of macrocyclic bisindolylmaleimides
Faul,Krumrich
, p. 2024 - 2033 (2007/10/03)
Three new approaches to the synthesis of macrocyclic bisindolylmaleimides 1-4 have been identified. Two strategies afford 8, the penultimate intermediate for the synthesis of 1-4, in 73% and 32% yield by intramolecular cyclization of 31 and 40, respectively. The optimum synthesis of 1 was achieved in nine steps and 15% yield by intramolecular formation of the macrocycle and maleimide in one step by reaction of the sodium indolate of 12 with methyl indole-3-glyoxylate 47. The mechanism of this reaction has been elucidated, using the trityl-protected derivative, to involve initial formation of the tricarbonyl imide 48, followed by irreversible alkylation of the indole nitrogen to generate the 17-membered macrocycle 49. Cyclization of 49 to hydroxymaleimide 50 and subsequent dehydration afforded 8a. This approach eliminated the problem of dimerization observed in the intramolecular cyclization reactions.
Intermediates and their use to prepare N,N'-bridged bisindolylmaleimides
-
, (2008/06/13)
This invention provides compounds of the formula: The invention further provides the use of this compound to prepare N,N'-bridged bisindolylmaleimides. Furthermore, the invention provides pharmaceutical formulations and the methods of use for inhibiting Protein Kinase C in mammals.
Synthesis of bisindolylmaleimides
-
, (2008/06/13)
The present invention provides a novel synthesis of the compounds of Formula (I): STR1 The compounds are produced in high yield and without utilizing expensive chromatographic separations. The synthesis is particularly advantageous because it is stereosel
