839711-73-8Relevant academic research and scientific papers
Total Synthesis of the Marine Natural Product Hemiasterlin by Organocatalyzed α-Hydrazination
Lang, Jan Hendrik,Jones, Peter G.,Lindel, Thomas
, p. 12714 - 12717 (2017/09/25)
An efficient synthesis of the potently cytotoxic marine peptide hemiasterlin is presented. The tetramethyltryptophan moiety is assembled by tert-prenylation of indole, followed by the high-yielding organocatalyzed α-hydrazination of a sterically congested aldehyde with excellent enantioselectivity. 2-Bromo-N-ethylpyridinium tetrafluoroborate (BEP)-mediated peptide coupling completes the synthesis, being the first approach that does not employ chiral auxiliaries. A novel phenonium-type rearrangement of the indole system occurred when subjecting dihydroxylated 3-tert-prenylindole to Mitsunobu conditions.
Novel pyrrolidine heterocycles as CCR1 antagonists
Merritt, J. Robert,James, Ray,Paradkar, Vidyadhar M.,Zhang, Chongwu,Liu, Ruiyan,Liu, Jinqi,Jacob, Biji,Chiriac, Camelia,Ohlmeyer, Michael J.,Quadros, Elizabeth,Wines, Pamela,Postelnek, Jennifer,Hicks, Catherine M.,Chen, Weiqing,Kimble, Earl F.,O'Brien, Linda,White, Nicole,Desai, Hema,Appell, Kenneth C.,Webb, Maria L.
supporting information; experimental part, p. 5477 - 5479 (2010/12/24)
A novel series of pyrrolidine heterocycles was prepared and found to show potent inhibitory activity of CCR1 binding and CCL3 mediated chemotaxis of a CCR1-expressing cell line. A potent, optimized triazole lead from this series was found to have acceptab
ORTHO PYRROLIDINE, BENZYL-SUBSTITUTED HETEROCYCLE CCR1 ANTAGONISTS FOR AUTOIMMUNE DISEASES and INFLAMMATION
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Page/Page column 28, (2009/04/24)
Compounds of the formula are disclosed. The compounds are CCR1 antagonists which are useful for the treatment and prevention of inflammatory and autoimmune diseases. Other embodiments are also disclosed.
PREPARATION OF TERAZOLE DERIVATIVES
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Page/Page column 28-29, (2010/11/25)
The invention relates to a process for the preparation of (S)-pyrrolidine-1H-tetrazole derivatives of formula (I), wherein R1, R2 and R3, independently of one another, represent hydrogen, halogen or an organic radical, in
Organocatalysis with proline derivatives: Improved catalysts for the asymmetric Mannich, nitro-Michael and aldol reactions
Cobb, Alexander J. A.,Shaw, David M.,Longbottom, Deborah A.,Gold, Johan B.,Ley, Steven V.
, p. 84 - 96 (2007/10/03)
Tetrazole and acylsulfonamide organocatalysts derived from proline have been synthesised and applied to the asymmetric Mannich, nitro-Michael and aldol reactions to give results that are superior to the proline-catalysed counterpart.
