75772-01-9Relevant academic research and scientific papers
CYCLIC COMPOUNDS AND METHODS OF USING SAME
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Page/Page column 385-386, (2021/07/02)
The present application relates to compounds of Formula (I), as defined herein, and pharmaceutically acceptable salts thereof which are MALT1 inhibitors. The present application also describes pharmaceutical composition comprising a compound of Formula (I), and pharmaceutically acceptable salts thereof, and methods of using the compounds and compositions for treating diseases, such as cancer, autoimmune disorders, and inflammatory disorders.
Method for preparing 3, 4-dihydroxyphenylethanol
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Paragraph 0058-0059; 0063-0064, (2020/06/20)
The invention discloses a method for preparing 3, 4-dihydroxyphenylethanol, which comprises the following steps: (1) preparing benzyloxymethyltriphenylphosphorus chloride, (2) preparing 3.4-dibenzyloxy benzaldehyde, (3) preparing 1, 2-dibenzyloxy-4-(2-benzyloxyvinyl)benzene, and (4) preparing 3, 4-dihydroxyphenylethanol. Compared with the prior art, the method has the advantages that 1, raw materials and reagents used in the method are lower in toxicity, safer, cheaper, easier to obtain and convenient to store, and the raw materials and operation cost are greatly reduced, 2, the method has fewreaction steps, is convenient to operate, and is easier for large-scale production, and 3, the method does not generate high-toxicity three wastes, so that the environmental pollution is reduced, andthe ecological environment is protected. Meanwhile, the yield of the prepared product is high and can reach 90% or above.
Synthesis and biochemical evaluation of lid-open D-amino acid oxidase inhibitors
Szilágyi, Bence,Hargitai, Csilla,Kelemen, ádám A.,Rácz, Anita,Ferenczy, Gy?rgy G.,Volk, Balázs,Keser?, Gy?rgy M.
supporting information, (2019/01/31)
Most of the known inhibitors of D-amino acid oxidase (DAAO) are small polar molecules recognized by the active site of the enzyme. More recently a new class of DAAO inhibitors has been disclosed that interacts with loop 218?224 at the top of the binding pocket. These compounds have a significantly larger size and more beneficial physicochemical properties than most reported DAAO inhibitors, however, their structure-activity relationship is poorly explored. Here we report the synthesis and evaluation of this type of DAAO inhibitors that open the lid over the active site of DAAO. In order to collect relevant SAR data we varied two distinct parts of the inhibitors. A systematic variation of the pendant aromatic substituents according to the Topliss scheme resulted in DAAO inhibitors with low nanomolar activity. The activity showed low sensitivity to the substituents investigated. The variation of the linker connecting the pendant aromatic moiety and the acidic headgroup revealed that the interactions of the linker with the enzyme were crucial for achieving significant inhibitory activity. Structures and activities were analyzed based on available X-ray structures of the complexes. Our findings might support the design of drug-like DAAO inhibitors with advantageous physicochemical properties and ADME profile.
A process for preparing N - Boc - 3 - pyrrolidine of formaldehyde (by machine translation)
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Paragraph 0045; 0046; 0050; 0051, (2019/02/04)
The invention discloses a method for preparing N - Boc - 3 - pyrrolidine of formaldehyde, comprising the following steps: (1) in the solvent is added in chloromethane-based [...] and triphenyl phosphate reaction, to obtain the benzyloxy methyl trityl chloride; (2) the benzyloxy methyl trityl chloride by adding solvent, under alkaline conditions, adding N - Boc - 3 - pyrrolidone reaction, to obtain compound N - Boc - 3 - benzyloxy methylene pyrrolidine; (3) high-pressure container for adding a solvent, N - Boc - 3 - benzyloxy methylene pyrrolidine and catalyst, hydrogenation reaction to obtain N - Boc - 3 - pyrrolidine methanol; (4) will be N - Boc - 3 - pyrrolidine methanol dissolved in dichloromethane solvent, adding Dess - Martin oxidizer to carry out oxidizing, get N - Boc - 3 - pyrrolidine formaldehyde. The method of the invention has the following advantages: the used raw materials low toxicity, easy, low cost, consumption, high yield, few by-products, easy large-scale production. (by machine translation)
Studies on the 6-homologation of β-D-idopyranosides
Hevey, Rachel,Ling, Chang-Chun
, p. 65 - 74 (2017/04/19)
β-D-Idopyranosides are interesting sugars because of their unusual conformational flexibility in the pyranosyl ring, and also their β-1,2-cis-anomeric configuration. Here we report our studies of the regioselective opening of 4,6-O-benzylidene-protected β-D-idopyranosides under reducing conditions, and the subsequent 6-homologation via Swern oxidation and Wittig olefination to afford a 6,7-dideoxy-β-D-ido-hept-6-enopyranoside. This olefination product was found to adopt predominantly 1C4 conformation in solution by NMR experiments, which places the vinyl group at a more sterically hindered axial position and creates difficulty in subsequent hydroborations.
IRAK INHIBITORS AND USES THEREOF
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Paragraph 00390; 00391, (2015/11/16)
The present invention provides quinazoline and quinoline compounds, compositions thereof, and methods of using the same. Also disclosed is the activity of such compounds as inhibitors of IRAK enzymes.
Synthetic Methods for the Preparation of D- and L-Pseudo-Sugars from D-Glucose
Barton, Derek H. R.,Gero, S.D.,Cleophax, Jeannine,Machado, Antonio Salustiano,Quiclet-Sire, Beatrice
, p. 1184 - 1186 (2007/10/02)
Starting from D-glucose and using Ferrier rearrangement to obtain the cyclohexanone (1), a convenient synthesis of crystalline pseudo-α-D-glucopyranose (15), its congeners (16) and (17), as well as their partially protected derivatives has been carried out.
