144001-42-3Relevant articles and documents
Radical 1,4-Aryl Migration Enabled Remote Cross-Electrophile Coupling of α-Amino-β-Bromo Acid Esters with Aryl Bromides
Chen, Shi-Lu,He, Jin,Hong, Yu,Li, Jin-Heng,Liu, Jian,Liu, Ting,Tang, Shi,Wang, Shuo-Wen,Xu, Zhen-Hua,Yu, Jian
supporting information, p. 21360 - 21367 (2021/08/23)
We report an unprecedented, efficient nickel-catalysed radical relay for the remote cross-electrophile coupling of β-bromo-α-benzylamino acid esters with aryl bromides via 1,4-aryl migration/arylation cascades. β-Bromo-α-benzylamino acid esters are consid
Hydrogen-Borrowing Alkylation of 1,2-Amino Alcohols in the Synthesis of Enantioenriched γ-Aminobutyric Acids
Hall, Christopher J. J.,Goundry, William R. F.,Donohoe, Timothy J.
supporting information, p. 6981 - 6985 (2021/03/01)
For the first time we have been able to employ enantiopure 1,2-amino alcohols derived from abundant amino acids in C?C bond-forming hydrogen-borrowing alkylation reactions. These reactions are facilitated by the use of the aryl ketone Ph*COMe. Racemisation of the amine stereocentre during alkylation can be prevented by the use of sub-stoichiometric base and protection of the nitrogen with a sterically hindered triphenylmethane (trityl) or benzyl group. The Ph* and trityl groups are readily cleaved in one pot to give γ-aminobutyric acid (GABA) products as their HCl salts without further purification. Both steps may be performed in sequence without isolation of the hydrogen-borrowing intermediate, removing the need for column chromatography.
Deoxyradiofluorination Reaction from β-Hydroxy-α-aminoesters: an Entry to [18F]Fluoroaminoesters under Mild Conditions
Morlot, Marine,Gourand, Fabienne,Perrio, Cécile
, p. 3751 - 3762 (2019/06/24)
We report the conversion of β-hydroxy-α-aminoesters derived from serine, α-methylserine or β-phenylserine to the corresponding [18F]fluorinated α or β-aminoesters by deoxyradiofluorination using [18F]fluoride. The method involved the
TETRACYCLIC HETEROARYL COMPOUNDS
-
Page/Page column 36; 41-42, (2020/01/10)
The specification relates to compounds of Formula (I) and pharmaceutically acceptable salts thereof. The specification also relates to processes and intermediates used for their preparation, pharmaceutical compositions containing them and their use in the treatment of cell proliferative disorders.
BTK INHIBITORS
-
Page/Page column 93, (2016/07/27)
Provided are Bruton's Tyrosine Kinase (Btk) inhibitor compounds according to Formula I, or pharmaceutically acceptable salts thereof, or pharmaceutical compositions comprising these compounds and their use in therapy. In particular, provided is the use of Btk inhibitor compounds of Formula I in the treatment of Btk mediated disorders.
HIV PROTEASE INHIBITORS
-
Page/Page column 24, (2015/07/07)
The present invention is directed to 5-heteroarylmorpholine derivatives and their use in the inhibition of HIV protease, the inhibition of HIV replication, the prophylaxis of infection by HIV, the treatment of infection by HIV, and the prophylaxis, treatment, and delay in the onset or progression of AIDS. The compounds and their salts can be employed as ingredients in pharmaceutical compositions, optionally in combination with other antivirals, immunomodulators, antibiotics or vaccines.
Nature-inspired total synthesis of (-)-fusarisetin A
Xu, Jing,Caro-Diaz, Eduardo J. E.,Trzoss, Lynnie,Theodorakis, Emmanuel A.
supporting information; experimental part, p. 5072 - 5075 (2012/05/07)
A concise, protecting group-free total synthesis of (-)-fusarisetin A (1) was efficiently achieved in nine steps from commercially available (S)-(-)-citronellal. The synthetic approach was inspired by our proposed biosynthesis of 1. Key transformations of our strategy include a facile construction of the decalin moiety that is produced via a stereoselective IMDA reaction and a one-pot TEMPO-induced radical cyclization/aminolysis that forms the C ring of 1. Our route is amenable to analogue synthesis for biological evaluation.
Synthesis of histidinoalanine: A comparison of β-lactone and sulfamidate electrophiles
Taylor, Carol M.,De Silva, Samanthi Thabrew
experimental part, p. 5703 - 5708 (2011/09/16)
Previous syntheses of histidinoalanine (HAL) have led to mixtures of regioisomers and/or stereoisomers. For example, opening of N-Cbz-d-serine- β-lactone (6) with Boc-l-His-OMe (5) gave a 2:1 mixture of τ- and π-regioisomers. The sulfamidate 10, derived f
CRYSTALLINE FORMS OF A PYRIDINE DERIVATIVE
-
Page/Page column 21-22, (2010/04/03)
The invention relates to 4-methylbenzenesulfonate salt of the compound of formula (I) in a crystalline form or in a solvate thereof, pharmaceutical formulations containing them, their use in therapy and processes for preparing the same.
Orthogonally protected glycerols and 2-aminodiols: Useful building blocks in heterocyclic chemistry
Ollivier, Anthony,Goubert, Marlene,Tursun, Ahmatjan,Canet, Isabelle,Sinibaldia, Marie-Eve
experimental part, p. 108 - 126 (2010/10/03)
The efficient synthesis of orthogonally protected glycerols, 2-aminopropane-1,3-diols and 2-aminobutane-1,4-diols that can constitute useful tools in heterocyclic chemistry, is reported. These interesting tri-functionalized small synthons were easily prepared from serine or aspartic acid. In addition, these substrates can be readily transformed into their iodide derivatives in very good yields. ARKAT USA, Inc.