- NOVEL JAK1 SELECTIVE INHIBITORS AND USES THEREOF
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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
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- PROCESSES OF PREPARING A JAK1 INHIBITOR AND NEW FORMS THERETO
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This invention relates to processes for preparing a JAKl inhibitor having Formula la: as well as new forms of the inhibitor.
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- Efficient and Selective Cu/Nitroxyl-Catalyzed Methods for Aerobic Oxidative Lactonization of Diols
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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.
- Xie, Xiaomin,Stahl, Shannon S.
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supporting information
p. 3767 - 3770
(2015/04/14)
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- Synthesis of Four Diastereomeric L-2-(Carboxycyclopropyl)glycines. Conformationally Constrained L-Glutamate Analogues
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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
- Shimamoto, Keiko,Ishida, Michiko,Shinozaki, Haruhikio,Ohfune, Yasufumi
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p. 4167 - 4176
(2007/10/02)
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- Conjugate addition to chiral γ-heterosubstituted δ-lactones as pivotal synthons from L-glutamic acid. Synthesis of an optically active lignan lactone; (-)-hinokinin
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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.
- Yoda,Naito,Takabe,Tanaka,Hosoya
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p. 7623 - 7626
(2007/10/02)
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- NEW ROUTES TO THE SYNTHESES OF CIS-α-(CARBOXYCYCLOPROPYL)GLYCINES FROM L-GLUTAMIC ACID. CONFORMATIONALLY RESTRICTED ANALOGUES OF THE EXCITATORY NEUROTRANSMITTER L-GLUTAMIC ACID
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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.
- Shimamoto, Keiko,Ohfune, Yasufumi
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p. 3803 - 3804
(2007/10/02)
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