174890-57-4Relevant academic research and scientific papers
Copper-Catalyzed Bisannulations of Malonate-Tethered O-Acyl Oximes with Pyridine, Pyrazine, Pyridazine, and Quinoline Derivatives for the Construction of Dihydroindolizine-Fused Pyrrolidinones and Analogues
Miao, Chun-Bao,Guan, Hong-Rong,Tang, Yihan,Wang, Kun,Ren, Wen-Long,Lyu, Xinyu,Yao, Changsheng,Yang, Hai-Tao
, p. 8699 - 8704 (2021/11/20)
A copper-catalyzed bisannulation reaction of malonate-tethered O-acyl oximes with pyridine, pyrazine, pyridazine, and quinoline derivatives has been developed for the concise synthesis of structurally novel dihydroindolizine-fused pyrrolidinones and their analogues. The present reaction shows excellent regioselectivity and stereoselectivity. Theoretical calculations reveal that the coordination effect of the carbonyl group in the nucleophilic substrate determines the excellent regioselectivity. Further functionalization of the generated dihydroindolizine-fused pyrrolidinone could be easily realized through substitution, Michael addition, selective aminolysis, and hydrolysis reactions.
Making method of t-butyloxycarboryl-3-(hydroxymethyl)-[1,2,3]triazole[1,5-a]piperidine-6-amide
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Paragraph 0007; 0008, (2017/10/13)
The invention relates to a synthesis method of t-butyloxycarboryl-3-(hydroxymethyl)-[1,2,3]triazole[1,5-a]piperidine-6-amide. The technical problem that a suitable industrial synthesis method does not exist at present is mainly solved. The synthesis method is divided into the following seven steps of firstly making (2-chloro-5-nitropyridine) and t-butyl ethyl malonate react in a solvent tetrahydrofuran under the action of NaH to obtain a compound 2; obtaining a compound 3 from the compound 2 under the action of trifluoroacetic acid; afterwards, subjecting the compound 3 to a hydrogenation reaction under the catalysis of palladium carbon to obtain a compound 4; carrying out t-butyloxycarboryl protection on the compound 4 to obtain a compound 5; making the compound 5 act with p-ABSA (p-Acetamidobenzenesulfonyl Azide) under the action of DBU (1,8-Diazabicyclo[5,4,0]undec-7-ene) to obtain a compound 6; reducing the compound 6 in the tetrahydrofuran by lithium aluminium tetrahydride to obtain a compound 7; subjecting the compound 7 to catalytic hydrogenation under the catalysis of wet palladium carbon to obtain a final compound 8.
HETEROCYCLIC COMPOUND
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Paragraph 0591, (2015/03/03)
The present invention provides an agent for the prophylaxis or treatment of autoimmune diseases (e.g., psoriasis, rheumatoid arthritis, inflammatory bowel disease, Sjogren's syndrome, Behcet's disease, multiple sclerosis, systemic lupus erythematosus etc.) and the like, which has a superior Tyk2 inhibitory action. The present invention relates to a compound represented by the formula wherein each symbol is as defined in the specification, or a salt thereof.
INHIBITORS OF CYTOMEGALOVIRUS
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Page/Page column 26, (2014/05/24)
Compounds of Formula (I) wherein n, R1, R1A, R2, R4 and Z are defined herein, are useful for the treatment of cytomegalovirus disease and/or infection.
QUINOLONE DERIVATIVES AS FIBROBLAST GROWTH FACTOR INHIBITORS
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Page/Page column 83, (2014/12/09)
Compounds of formula (Ι') that are Fibroblast Growth Factor Inhibitors (FGFR) and are therefore useful for the treatment of diseases treatable by inhibition of FGFR are disclosed. Also disclosed are pharmaceutical compositions containing such compounds and processes for preparing such compounds.
SUBSTITUTED HETEROAROMATIC PYRAZOLE-CONTAINING CARBOXAMIDE AND UREA DERIVATIVES AS VANILLOID RECEPTOR LIGANDS
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Page/Page column 141; 142, (2013/03/26)
The invention relates to substituted heteroaromatic pyrazole-containing carboxamide and urea derivatives as vanilloid receptor ligands, to pharmaceutical compositions containing these compounds and also to these compounds for use in the treatment and/or prophylaxis of pain and further diseases and/or disorders.
Substituted Heteroaromatic Pyrazole-Containing Carboxamide and Urea Compounds as Vanilloid Receptor Ligands
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Paragraph 0797, (2013/03/26)
Substituted heteroaromatic pyrazole-containing carboxamide and urea compounds as vanilloid receptor ligands, pharmaceutical compositions containing these compounds and also to a method of using these compounds for treating and/or inhibiting pain and further diseases and/or disorders.
INDAZOLECARBOXAMIDE DERIVATIVES AS 5HT4 RECEPTOR AGONISTS
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Page/Page column 25, (2008/06/13)
This invention relates to compounds of the formula (I): or pharmaceutically acceptable salts thereof, wherein: R1, R2, R3, A and m are each as described herein and compositions containing such compounds and the use of such
INHIBITORS OF C-FMS KINASE
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Page/Page column 68, (2008/06/13)
The invention is directed to compounds of Formula I: wherein Z, X, J, R2 and W are set forth in the specification, as well as solvates, hydrates, tautomers and pharmaceutically acceptable salts thereof, that inhibit protein tyrosine kinases, especially c-fms kinase. Methods of treating autoimmune diseases; and diseases with an inflammatory component; treating metastasis from ovarian cancer, uterine cancer, breast cancer, colon cancer, stomach cancer, hairy cell leukemia and non-small lung carcinoma; and treating pain, including skeletal pain caused by tumor metastasis or osteoarthritis, or visceral, inflammatory, and neurogenic pain; as well as osteoporosis, Paget's disease, and other diseases in which bone resorption mediates morbidity including arthritis, prosthesis failure, osteolytic sarcoma, myeloma, and tumor metastasis to bone with the compounds of Formula I, are also provided.
