155742-48-6Relevant articles and documents
Synthesis and orthogonal functionalization of oxazolo[5′,4′:4,5]pyrano[2,3-b]pyridine by intra- and intermolecular Pd-catalyzed direct C-H bond heteroarylation
Théveau, Laure,Schneider, Cédric,Querolle, Olivier,Meerpoel, Lieven,Levacher, Vincent,Hoarau, Christophe
, p. 3459 - 3468 (2016)
The construction and subsequent orthogonal functionalization of a hitherto unknown oxazolo[5′,4′:4,5]pyrano[2,3-b]pyridine are reported. A palladium-catalyzed direct C-H bond functionalization methodology was used to build the tricyclic scaffold as well as to achieve the subsequent C-H bond functionalization at the C-2 position of the oxazole unit with various (hetero)aryl iodides. Remarkably, selective C-H construction and functionalization procedures preserve the chorine atom on the pyridine moiety offering a late-stage substitution site to progress drug design.
Preparation method of 2-(oxazolyl) ethylamine
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Paragraph 0127; 0128, (2019/12/25)
The invention discloses a preparation method of 2-(oxazolyl) ethylamine. According to the preparation method of 2-(oxazolyl) ethylamine, oxazole ring-opening side reaction is effectively avoided, therepeatability is good, the conversion rate and yield are high, and purification is easy; reaction conditions are mild, safety is high, potential safety hazards to operators are reduced, the operationsafety level of production is reduced, and the method is environmentally friendly; the obtained 2-(oxazolyl) ethylamine product is high in purity and good in quality, and industrialization is facilitated.
AMINOPYRIDINE DERIVATIVES AS PHOSPHATIDYLINOSITOL PHOSPHATE KINASE INHIBITORS
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Paragraph 0743, (2019/07/13)
The invention relates to inhibitors of PI5P4K inhibitors useful in the treatment of cancers, neurodegenerative diseases, inflammatory disorders, and metabolic diseases, having the Formula: (I) where A, B, R1, X1, X2, and W are described herein.
SMALL MOLECULE ACTIVATORS OF NICOTINAMIDE PHOSPHORIBOSYLTRANSFERASE (NAMPT) AND USES THEREOF
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Paragraph 00369, (2018/08/03)
Provided herein are small molecule activators of Nicotinamide Phosphoribosyltransferase (NAMPT), compositions comprising the compounds, and methods of using the compounds and compositions.
AMINOPYRAZINE COMPOUNDS WITH A2A ANTAGONIST PROPERTIES
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Paragraph 0159, (2016/06/21)
Disclosed are compounds of Formula A and Formula A-1, or a salt thereof, and pharmaceutical formulations (pharmaceutical compositions) comprising those compounds, or a salt thereof; wherein "R1", "RA-1", "R2", "R3", and "Het" are defined herein above, which compounds are believed suitable for use in selectively antagonizing the A2a receptors, for example, those found in high density in the basal ganglia. Such compounds and pharmaceutical formulations are believed to be useful in treatment or management of neurodegenerative diseases, for example, Parkinson's disease, or movement disorders arising from use of certain medications used in the treatment or management of Parkinson's disease.
Chemical Compounds
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Page/Page column 47, (2009/07/17)
This invention relates to non-steroidal compounds that are modulators of androgen, glucocorticoid, mineralocorticoid, and progesterone receptors, and also to the methods for the making and use of such compounds.
NOVEL PHARMACEUTICALS
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Page/Page column 57, (2010/11/28)
The present invention relates to immune response modifiers of formula (I), which act selectively through agonism, of Toll-Like Receptors (TLRs), uses thereof, processes for the preparation thereof, intermediates used in the preparation thereof and compositions containing said inhibitors. These inhibitors have utility in a variety of therapeutic areas including the treatment of infectious disease such as Hepatitis (e.g. HCV, HBV), genetically related viral infection and cancer.
BICYCLONONENE DERIVATIVES AS RENIN INHIBITORS
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Page/Page column 34, (2008/06/13)
The invention relates to novel bicyclononene derivatives of Formula (I); and the use thereof as active ingredients in the preparation of pharmaceutical compositions. The invention also concerns related aspects including processes for the preparation of the compounds, pharmaceutical compositions containing one or more of those compounds and especially their use as inhibitors of renin.
FUSED QUINOLINE DERIVATIVE AND USE THEREOF
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Page/Page column 109, (2008/06/13)
The present invention aims at provision of a quinoline derivative having a neurokinin 2 (NK2) receptor antagonistic action and relates to a compound represented by the formula (I) wherein Rl is a hydrogen atom and the like; R2 is a hydrogen atom, a hydrocarbon group optionally having substituent(s) and the like; R3 is unsubstituted (i.e., absence), a hydrogen atom and the like; R4 and R5 are the same or different and each is a hydrogen atom, a hydrocarbon group optionally having substituent(s), and the like; R6is (cyclic group optionally having substituent(s)) -carbonyl, and the like; R7, R8,R9 and R10 are the same or different and each is a hydrogen atom, halogen and the like; or R7and R8,R8 and R9,and R9 and R10 may form a ring together with the adjacent carbon atoms; n is an integer of 1 to 5; --- represents unsubstituted (i.e., absence) or a single bond; and --- represents a single bond or a double bond, or a salt thereof, and the like.
4-Bromomethyl-2-chlorooxazole - A versatile oxazole cross-coupling unit for the synthesis of 2,4-disubstituted oxazoles
Young, Gail L.,Smith, Stephen A.,Taylor, Richard J.K.
, p. 3797 - 3801 (2007/10/03)
The synthesis of the novel oxazole building block, 4-bromomethyl-2- chlorooxazole, and its palladium-catalysed cross-coupling reactions to make a range of 2,4-disubstituted oxazoles, is described. Selectivity for the 4-bromomethyl position is observed, with Stille coupling effected in good to excellent yields, or Suzuki coupling in moderate yields, to provide a range of 4-substituted-2-chlorooxazoles. Subsequent coupling at the 2-chloro-position can be achieved through either Stille or Suzuki reactions in excellent yields.