591769-05-0Relevant articles and documents
HSP90 INHIBITORS AND USES THEREOF
-
Paragraph 00178; 00198; 00207, (2020/11/23)
Herein is described the design and synthesis of resorcylate aminopyrazole compounds. These compounds show broad, potent and fungal-selective Hsp90 inhibitory activity. These compounds also find use in treating Hsp90 related deseases.
Oxa-Michael Addition to α,β-Unsaturated Nitriles: An Expedient Route to γ-Amino Alcohols and Derivatives
Guo, Beibei,Zijlstra, Douwe S.,de Vries, Johannes G.,Otten, Edwin
, p. 2868 - 2872 (2018/07/24)
Water addition to α,β-unsaturated nitriles would give facile access to the β-hydroxy-nitriles, which in turn can be hydrogenated to the γ-amino alcohols. We have previously shown that alcohols readily add in 1,4-fashion to these substrates using Milstein's Ru(PNN) pincer complex as catalyst. However, attempted water addition to α,β-unsaturated nitriles gave the 3-hydroxynitriles in mediocre yields. On the other hand, addition of benzyl alcohol proceeded in excellent yields for a variety of β-substituted unsaturated nitriles. Subsequent treatment of the benzyl alcohol addition products with TMSCl/FeCl3 resulted in the formation of 3-hydroxy-alkylnitriles. The 3-benzyloxy-alkylnitriles obtained from oxa-Michael addition also could be hydrogenated directly in the presence of acid to give the amino alcohols as their HCl salts in excellent yields. Hydrogenation under neutral conditions gave a mixture of the secondary and tertiary amines. Hydrogenation in the presence of base and Boc-anhydride gave the orthogonally bis-protected amino alcohols, in which the benzyl ether can subsequently be cleaved to yield Boc-protected amino alcohols. Thus, a variety of molecular scaffolds with a 1,3-relationship between O- and N-functional group is accessible starting from oxa-Michael addition of benzyl alcohol to α,β-unsaturated nitriles.
JANUS KINASE INHIBITORS FOR TREATMENT OF DRY EYE AND OTHER EYE RELATED DISEASES
-
Paragraph 0111, (2016/03/05)
Methods, kits, and compositions for treating dry eye disorders and other related eye diseases are provided, wherein the methods, kits, and compositions utilize a JAK inhibitor.
JAK kinase inhibitor containing 4-aminopyrazole structure, preparation method and application thereof
-
Paragraph 0110; 0111, (2016/10/07)
The invention relates to a JAK kinase inhibitor containing a 4-aminopyrazole structure, a preparation method and an application thereof. Compounds of the series have structures shown in a general formula (I) or a general formula (II). The invention also provides the preparation method of the kinase inhibitor, and the application of the kinase inhibitor in preparation of medicines for preventing or treating inflammation, tumor and blood-related diseases.
Five-And-Six-Membered Heterocyclic Compound, And Preparation Method, Pharmaceutical Composition And Use Thereof
-
Paragraph 0122; 0125; 0126, (2015/12/07)
A five-and-six-membered heterocyclic compound as represented by general formula I, pharmaceutically acceptable salt, metabolite, metabolic precursors or drug precursors thereof, preparation method, pharmaceutical composition, and use thereof; the five-and-six-membered heterocyclic compound has activity as a Janus kinase (JAK) inhibitor, and can be used to prepare drugs for treating diseases caused by the abnormal activity of kinase, such as cell proliferation diseases like cancer.
HETEROCYCLIC COMPOUNDS AS JANUS KINASE INHIBITORS
-
Page/Page column 147-148, (2011/04/18)
The invention provides compounds of formula (I) or a salt thereof as described herein. The invention also provides pharmaceutical compositions comprising a compound of formula (I), processes for preparing compounds of formula (I), intermediates useful for preparing compounds of formula I and therapeutic methods for suppressing an immune response or treating cancer or a hematologic malignancy using compounds of formula (I).
Wadsworth-Emmons reaction: The unique catalytic reaction by a solid base
Choudary, Boyapati M.,Kantam, Mannepalli L.,Reddy, Chinta Reddy V.,Bharathi, Balagam,Figueras, Francois
, p. 191 - 200 (2007/10/03)
The near-stoichiometric amount of bases is used both in laboratory and industry in Wadsworth-Emmons (WE) reactions, since the by-product, (EtO) 2P(O)OH, formed in the reaction neutralizes the base into an inert salt. A strategy to design, develop, and evolve the recyclable Mg-Al-hydrotalcite-OtBu (HT-OtBu) by the interaction of KOtBu with the calcined hydrotalcite that transforms a well-defined stoichiometric WE reaction into a catalytic one in an effort to minimize the quantum of effluents released and reduce the cost of the process is described here. HT-OtBu is found to be an efficient solid base for WE reactions for the simple synthesis of α,β-unsaturated esters and nitriles for the first time. The HT-OtBu, composed of various ratios of Mg/Al (i.e., 2, 2.5, and 3) and different contents of tBuO - (Mg/Al:3), and their precursors were prepared and well characterized to draw a correlation between structure and reactivity of the hydrotalcites in WE reactions.
