125982-23-2Relevant articles and documents
NOVEL JAK1 SELECTIVE INHIBITORS AND USES THEREOF
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, (2018/04/21)
The new 1H-furo[3,2-b]imidazo[4,5-d]pyridine derivatives are selective Jak1 kinase inhibitors useful in treating disorders related to Jak1 activities such as autoimmune diseases or disorders, inflammatory diseases or disorders, and cancer or neoplastic di
PROCESSES OF PREPARING A JAK1 INHIBITOR AND NEW FORMS THERETO
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, (2015/11/24)
This invention relates to processes for preparing a JAKl inhibitor having Formula la: as well as new forms of the inhibitor.
Efficient and Selective Cu/Nitroxyl-Catalyzed Methods for Aerobic Oxidative Lactonization of Diols
Xie, Xiaomin,Stahl, Shannon S.
supporting information, p. 3767 - 3770 (2015/04/14)
Cu/nitroxyl catalysts have been identified that promote highly efficient and selective aerobic oxidative lactonization of diols under mild reaction conditions using ambient air as the oxidant. The chemo- and regioselectivity of the reaction may be tuned by changing the identity of the nitroxyl cocatalyst. A Cu/ABNO catalyst system (ABNO = 9-azabicyclo[3.3.1]nonan-N-oxyl) shows excellent reactivity with symmetrical diols and hindered unsymmetrical diols, whereas a Cu/TEMPO catalyst system (TEMPO = 2,2,6,6-tetramethyl-1-piperidinyl-N-oxyl) displays excellent chemo- and regioselectivity for the oxidation of less hindered unsymmetrical diols. These catalyst systems are compatible with all classes of alcohols (benzylic, allylic, aliphatic), mediate efficient lactonization of 1,4-, 1,5-, and some 1,6-diols, and tolerate diverse functional groups, including alkenes, heterocycles, and other heteroatom-containing groups.
Synthesis of Four Diastereomeric L-2-(Carboxycyclopropyl)glycines. Conformationally Constrained L-Glutamate Analogues
Shimamoto, Keiko,Ishida, Michiko,Shinozaki, Haruhikio,Ohfune, Yasufumi
, p. 4167 - 4176 (2007/10/02)
To determine what conformations of L-glutamate (L-Glu) activate that compound's different receptors in the mammalian central nervous system, four diastereochemically L-2-(carboxycyclopropyl)glycines, 1-4, which are conformationally constrained analogues o
Conjugate addition to chiral γ-heterosubstituted δ-lactones as pivotal synthons from L-glutamic acid. Synthesis of an optically active lignan lactone; (-)-hinokinin
Yoda,Naito,Takabe,Tanaka,Hosoya
, p. 7623 - 7626 (2007/10/02)
Asymmetric induction in conjugate addition of new chiral γ-heterosubstituted-α, β-unsaturated δ-lactones from L-glutamic acid was accomplished in high diastereoselectivity with the formation of trans-(R,S)-adducts and was disclosed to serve as a versatile procedure for the asymmetric synthesis of antileukemic lignan lactones.
NEW ROUTES TO THE SYNTHESES OF CIS-α-(CARBOXYCYCLOPROPYL)GLYCINES FROM L-GLUTAMIC ACID. CONFORMATIONALLY RESTRICTED ANALOGUES OF THE EXCITATORY NEUROTRANSMITTER L-GLUTAMIC ACID
Shimamoto, Keiko,Ohfune, Yasufumi
, p. 3803 - 3804 (2007/10/02)
Potent neuroactive amino acids, (2S,2S,4R) and (2S,3R,4S) isomers of α-(carboxycyclopropyl)glycines (CCG-III and CCG-IV), were synthesized from L-glutamic acid via a palladium(II) catalyzed cyclopropanation of the α,β-unsaturated pyrrolidone and γ-amino-δ-lactone derivatives, respectively.
