194933-51-2Relevant academic research and scientific papers
Enantioselective Construction of Octahydroquinolines via Trienamine-Mediated Diels-Alder Reactions
Inoshita, Taichi,Goshi, Kei,Morinaga, Yuka,Umeda, Yuhei,Ishikawa, Hayato
, p. 2903 - 2907 (2019)
A trienamine-mediated asymmetric Diels-Alder reaction using a 5-nitro-2,3-dihydro-4-pyridone derivative as a dienophile in the presence of a secondary amine organocatalyst derived from cis-hydroxyproline was discovered. The reaction provides optically act
HYDROXYPROLINE DERIVATIVE
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Paragraph 0175, (2017/01/02)
PROBLEM TO BE SOLVED: To provide hydroxyproline derivatives useful as catalysts for e.g. Michael addition reactions and their salts. SOLUTION: Hydroxyproline derivatives having a relative configuration of formula (I) and their salts are provided. In formu
PHENYL AMINO PYRIMIDINE BICYCLIC COMPOUNDS AND USES THEREOF
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Page/Page column 59, (2014/01/17)
The present invention relates to phenyl amino pyrimidine bicyclic compounds formula (I) which are inhibitors of protein kinases including JAK kinases. In particular the compounds are active against JAK1, JAK2, JAK3 and TYK2 kinases. The kinase inhibitors can be used in the treatment of kinase associated diseases such as immunological and inflammatory diseases including organ transplants; hyperproliferative diseases including cancer and myeloproliferative diseases; viral diseases; metabolic diseases; and vascular diseases.
VLA-4 INHIBITOR
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Page/Page column 91, (2010/02/15)
A compound which selectively inhibits bonding between a ligand and α4β1 integrin (VLA-4); a process for producing the compound; and a medicine containing the compound. The compound is one represented by, e.g., the formula (I) or a salt thereof. Also provided is a preventive and/or therapeutic agent which contains the compound or salt as a major component and is effective against diseases attributable to cell adhesion, such as, e.g., inflammatory reaction, autoimmune disease, cancer metastasis, bronchial asthma, nasal obstruction, diabetes, arthritis, psoriasis, multiple sclerosis, inflammatory intestinal disease, and rejection reaction in transplantation. (In the formula, Y1 represents arylene, etc.; V1 represents aryl, etc.; and R11 to R14 each represents H, OH, halogeno, etc.)
Developing microcolin A analogs as biological probes
Mandal, Amit K.,Hines, John,Kuramochi, Kouji,Crews, Craig M.
, p. 4043 - 4047 (2007/10/03)
Three microcolin A and B analogs have been synthesized. Their biological activity profiles were evaluated against several cell lines, revealing the existence of a structural determinant whose role in mediating the antiproliferative effect of the microcoli
Synthesis of Microcolin B, a Potent New Immunosuppressant Using an Efficient Mixed Imide Formation Reaction
Andrus, Merritt B.,Li, Wenke,Keyes, Robert F.
, p. 5542 - 5549 (2007/10/03)
Microcolin B, a potent new immunosuppressant isolated from blue-green alga Lyngbya majuscula off the Venezuelan coast, has been made using a methyl-directed asymmetric hydrogenation reaction with rhodium on alumina catalyst on lactone 4 for the synthesis of the key (R,R)-2,4-dimethyl-octanoic acid fragment 1. A new, direct mixed imide formation reaction was also developed for the production of the unusual prolylpyrrolen-2-one 2 portion of microcolin. The pentafluorophenyl ester of CBZ-proline 5 was reacted with the lithium imidate of lactam 6, providing the mixed imide in 80% yield. Coupling of acid 1 with the N-terminus of the tripeptide, followed by coupling with pyrrolylproline 2, gave microcolin B. The new mixed-imide forming reaction was also applied to a formal total synthesis of microcolin A. The pentafluorophenyl ester of TBS-protected cis-hydroxyproline was coupled with lactam 6, and the resultant imide was converted to the key pyrrolylproline made previously for microcolin A.
