153198-06-2Relevant articles and documents
METHODS AND COMPOUNDS FOR TREATMENT OF LYMPHOCYTE-RELATED DISEASES AND CONDITIONS
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Page/Page column 34, (2016/12/22)
Methods for treatment of lymphocyte-related diseases and conditions, such as cancer and automimmune diseases, are provided. The methods comprise administration of an effective amount of an oligomer to a patient in need thereof, wherein the oligomer comprises, inter alia, at least one intersubunit linkage having the following structure: wherein R1, L1, X, Y and Z are as defined herein.
Mild deprotection of primary N-(p-toluenesulfonyl) amides with SmI 2 following trifluoroacetylation
Moussa, Ziad,Romo, Daniel
, p. 3294 - 3298 (2008/09/17)
A mild deprotection method for notoriously difficult to unmask primary N-(p-toluenesulfonyl) amides was developed during our total synthesis studies toward the marine toxin, gymnodimine. The deprotection occurs at low temperature (-78 °C) under mild conditions by initial activation of the nitrogen with a trifluoroacetyl group, followed by reductive cleavage of the p-toluenesulfonyl group with samarium diiodide. The substrate scope and functional group tolerance of this useful N-S cleavage process, which builds on related cleavage processes of other nitrogen-heteroatom bonds, is explored. Georg Thieme Verlag Stuttgart.
18F-labeled benzamides for studying the dopamine D2 receptor with positron emission tomography
Mach,Leudtke,Unsworth,Boundy,Nowak,Scripko,Elder,Jackson,Hoffman,Evora,Rao,Molinoff,Childers,Ehrenkaufer
, p. 3707 - 3720 (2007/10/02)
Two series of (N-benzylpiperidin-4-yl)- and (9-azabicyclo[3.3.1]nonan- 3β-yl)benzamides were prepared, and in vitro binding assays were used to measure the affinity of these compounds for dopamine D2, dopamine D3, serotonin 5-HT2, and α2-adrenergic receptors. The results of these studies indicated compounds 23, 26b, and 34 have the selectivity needed for in vivo studies of the D2 (and possibly D3) receptors. 18F-Labeled analogues of 23, 26b and 34 were prepared by N-alkylation of the corresponding desbenzyl precursors with [18F]-4-fluorobenzyl iodide. Preliminary in vivo studies demonstrated that [18F]-23 and [18F]-26b are suitable candidates for further evaluation in positron emission tomography imaging studies. The slow rate of washout of [18F]-34 from nondopaminergic regions and its comparatively high lipophilicity indicates that this compound may not be suitable for imaging studies because of a high level of nonspecific binding.