55227-00-4Relevant articles and documents
NOVEL COMPOUNDS
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, (2016/02/26)
A compound of formula (I) or a pharmaceutically acceptable derivative thereof, (formula 1) wherein R1,R2, R3, R4, R5, X, m and n are defined in the specification; a process for preparing such compounds; a pharmaceutical composition comprising such compounds; and the use of such compounds in medicine.
Enantioselective synthesis of the protein phosphatase inhibitor (-)-motuporin
Hu, Tao,Panek, James S.
, p. 11368 - 11378 (2007/10/03)
A highly convergent asymmetric synthesis of the protein phosphatase inhibitor motuporin 1a is described. Synthesis and coupling of the individual peptide fragments [34 + -35 → 51] followed by macrocyclization afforded the fully protected motuporin precursor 33, which is converted to the natural product by dehydration and ester hydrolysis, Six of the eight stereogenic centers associated with the natural product were introduced using asymmetric crotylsilane bond construction methodology. Our approach features an efficient Pd(0)-catalyzed cross-coupling reaction between a configurationally well-defined vinyl zinc intermediate 22 and an (E)-vinyl iodide 7, which afforded compound 43, resulting in the construction of the trisubstituted (E,E)-diene system of the motuporin side chain. Improved reaction conditions for macrocyclization in the formation of 33 are also detailed.
Synthesis of functionalised cyclic pentapeptide analogues of the serine-threonine protein phosphatase inhibitor nodularin
Mehrotra, Amit P.,Gani, David
, p. 6915 - 6918 (2007/10/03)
A generic synthesis of cyclic peptidic analogues of nodularin incorporating suitable functionality for synthetic elaboration is described, providing access to new protein phosphatase inhibitors.
