20265-37-6Relevant articles and documents
Peptide thioacylation with high stereochemical preservation
Hoeg-Jensen, Thomas,Holm, Arne,Sorensen, Hilmer
, p. 383 - 387 (1996)
A dipeptide thioamide model system, Boc-Leu-ψ[CSNH]-Met-OMe, was used for evaluating the preservation of amino acid stereochemistry during thioacylation utilizing amino monothio acids. The LL and DL peptide diastereomers were separated by use of high performance capillary electrophoresis (micellar electrokinetic capillary chromatography). The described thioacylation method combines monothio acids with coupling reagents of the PyBOP-family for generating active thiono esters with low-levels of enantiomerisation ( 2%). The best results in terms of stereochemical preservation and yield were obtained with PyNOP, a 6-nitro analog of PyBOP. The successful activation of thiobenzoic acid with all four coupling reagents extended the scope of the method to include aryl monothio acids.
A convenient room temperature ipso-nitration of arylboronic acid catalysed by molecular iodine using zirconium oxynitrate as nitrating species: An experimental and theoretical investigation
Mahanta, Abhijit,Gour, Nanda Kishor,Sarma, Plaban Jyoti,Borah, Raju Kumar,Raul, Prasanta Kumar,Deka, Ramesh Chandra,Thakur, Ashim Jyoti,Bora, Utpal
, (2019/05/15)
A simple and convenient protocol has been developed for ipso-nitration of arylboronic acid catalysed by molecular iodine at room temperature, using zirconium oxynitrate as the nitrating species. The protocol is applicable to electronically diverse aryl- and heteroarylboronic acid moieties under mild reaction conditions with good to excellent isolated yields. Furthermore, a theoretical investigation has been performed for the same reaction, and reaction profiles are modelled using modern density functional theory (DFT). DFT-based results support the experimentally observed results.
NOVEL COMPOUNDS FOR MODULATION OF ROR-GAMMA ACTIVITY
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Paragraph 00586, (2014/03/22)
The present invention relates to aryl sulfones and related compounds that are modulators of ROR-gamma receptors. The invention also provides pharmaceutical compositions comprising these modulators, and methods of modulating ROR-gamma receptors using them. Also provided are methods of using aryl sulfones and related compounds as modulators of ROR-gamma to treat ROR-gamma mediated diseases
The design of efficient and selective routes to pyridyl analogues of 3-oxo-3,4-dihydro-2H-1,4-(benzothiazine or benzoxazine)-6-carbaldehydes
Brooks, Gerald,Dabbs, Steven,Davies, David T.,Hennessy, Alan J.,Jones, Graham E.,Markwell, Roger E.,Miles, Timothy J.,Owston, Nathan A.,Pearson, Neil D.,Peng, Tony W.
scheme or table, p. 5035 - 5037 (2011/01/04)
This Letter describes the synthesis of challenging pyridyl analogues of 3-oxo-3,4-dihydro-2H-1,4-(benzothiazine or benzoxazine)-6-carbaldehydes. The six different routes described are high yielding, contain no major purification issues and have been used to give gram quantities of each aldehyde.
THIENOPYRIMIDINE COMPOUNDS AND USE THEREOF
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Page/Page column 27, (2010/02/14)
The present invention provides a compound represented by the formula: wherein R1 is a C1-4 alkyl; R2 is (1) a 5- to 7-membered nitrogen-containing heterocyclic group which may have a substituent selected from the group consisting of (1') a halogen, (2') a hydroxy group, (3') a C1-4 alkyl and (4') a C1-4 alkoxy, (2) a phenyl which may have a substituent selected from the group consisting of (1') a halogen, (2') a C1-4 alkoxy-C1-4 alkyl, (3') a mono-C1-4 alkyl-carbamoyl-C1-4 alkyl, (4') a C1-4 alkoxy and (5') a mono-C1-4 alkylcarbamoyl-C1-4 alkoxy, or the like; R3 is a C1-4 alkyl; R4 is a C1-4 alkoxy, or the like; n is an integer of 1 to 4; or a salt thereof, as a thienopyrimidine compound having gonadotropin-releasing hormone antagonistic activity.
Synthesis of a beta-turn forming depsipeptide for hydrogen bond mediated electron transfer studies
Williamson, David A.,Bowler, Bruce E.
, p. 12357 - 12372 (2007/10/03)
Hydrogen bonds are believed to play an important role in the mediation of electron transfer processes in proteins. A porphyrin/depsipeptide/p-benzoquinone molecule has been synthesized to help understand this role of hydrogen bond mediated electron transfer in proteins. The synthesis, room temperature folding conformation, and steady-state electron transfer are described.
Imidazopyridazines. XVIII. Syntheses and Central Nervous System Activities of Some 6-, 7- and 8-(Chloro and methoxy)imidazopyridine Analogues
Barlin, Gordon B.,Davies, Les P.,Harrison, Peter W.
, p. 1031 - 1038 (2007/10/02)
Syntheses are reported for some 2-aryl-3-(benzamidomethyl and methoxy)-6(7 and 8)-chloro- and 6(and 8)-methoxy-imidazopyridines.In tests of the ability of these compounds to displace diazepam from rat brain membrane, those with 6-chloro and 6-methoxy groups bound most strongly, and relatively small differences only were observed between corresponding imidazopyridines and imidazopyridazines.
