1803033-61-5Relevant articles and documents
Asymmetric Phase-Transfer Catalytic aza-Michael Addition to Cyclic Enone: Highly Enantioselective and Diastereoselective Synthesis of Cyclic 1,3-Aminoalcohols
Lee, Jaeyong,Ban, Jeong Woo,Kim, Jeongseok,Yang, Sehun,Lee, Geumwoo,Dhorma, Lama Prema,Kim, Mi-Hyun,Ha, Min Woo,Hong, Suckchang,Park, Hyeung-Geun
, p. 1647 - 1651 (2022/03/03)
The highly enantioselective aza-Michael reaction of tert-butyl β-naphthylmethoxycarbamate to cyclic enones has been accomplished by using a new cinchona alkaloid derived C(9)-urea ammonium catalyst under phase-transfer catalysis conditions with up to 98% ee at 0 °C. The resulting aza-Michael adducts can be converted to versatile intermediates by selective deprotection and the cyclic 1,3-aminoalcohols by diastereoselective reduction with up to 32:1, which have been widely used as important pharmacophores in pharmaceutical development.
PYRROLO[2,3-d]PYRIMIDINE COMPOUND OR SALT THEREOF
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Paragraph 0117; 0118, (2018/06/15)
Provided are a novel compound or a salt thereof, and a pharmaceutical composition comprising the same, which selectively and strongly inhibit JAK3, exhibit an excellent activity for suppressing the growth of human peripheral blood monocytes and an excellent oral absorbability, and exhibits an activity of inhibiting IL-2-induced IFN-γ production in vivo. A compound represented by formula (I) [wherein X represents -CH=CH-, -NH-, a sulfur atom or an oxygen atom; and n represents an integer of 0 to 2], or a salt thereof.
INHIBITORS OF CYCLIN-DEPENDENT KINASE 7 (CDK7)
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, (2016/12/26)
The present invention provides novel compounds of Formula (I) and pharmaceutically acceptable salts, solvates, hydrates, tautomers, stereoisomers, isotopically labeled derivatives, and compositions thereof. Also provided are methods and kits involving the compounds or compositions for treating or preventing proliferative diseases (e.g., cancers (e.g., leukemia, melanoma, multiple myeloma), benign neoplasms, angiogenesis, inflammatory diseases, autoinflammatory diseases, and autoimmune diseases) in a subject. Treatment of a subject with a proliferative disease using a compound or composition of the invention may inhibit the aberrant activity of cyclin-dependent kinase (e.g., CDK7), and therefore induce cellular apoptosis and/or inhibit transcription in the subject.