169229-06-5Relevant articles and documents
Improved synthesis of sterically encumbered heteroaromatic biaryls from aromatic β-keto esters
Rosen, Brandon R.,Ul Sharif, Ehesan,Miles, Dillon H.,Chan, Nicholas S.,Leleti, Manmohan R.,Powers, Jay P.
supporting information, (2020/03/25)
A protocol for the synthesis of hindered 4-aryl 2-aminopyrimidines from β–keto esters is described. The process employs trifluoroethanol as an essential additive to promote the guanidine condensation reaction, enabling the synthesis of 25 aryl- and heteroaryl substituted aminopyrimidines in good yields and high purities with no column chromatography. The conditions described herein are readily scalable and have been employed in the large-scale synthesis of the clinical A2a/A2bR antagonist AB928.
BICYCLIC HYDROXAMIC ACIDS USEFUL AS INHIBITORS OF MAMMALIAN HISTONE DEACETYLASE ACTIVITY
-
Page/Page column 92, (2017/07/14)
A compound of formula (Ia) or (Ib) or a pharmaceutically acceptable salt thereof. The compound is an inhibitor of a histone deacetylase, and as such is useful in terepy, e.g. in the treatment of autoimmune disorders, mental disorders, neurodegenerative disorders, and hyperproliferative disorders.
Tetrazolinone compound and application for same
-
Paragraph 0628; 0629, (2016/10/08)
Provided is a tetrazolinone compound given by formula (1) (wherein E represents the following group E16 or the like; Y represents -O-CH2- or the like; Q represents the following group Q46 or the like; R8 represents a C1-C6 alkyl group; R3, R30, and R31 may be the same or different, and represent hydrogen atoms or the like; A represents a C6-C16 aryl group or the like, optionally having one or more atoms or groups selected from the group P1; R5 represents a C1-C3 alkyl group; and X represents an oxygen or sulfur atom), and having exceptional efficacy in controlling harmful organisms.
ANTI-FIBROTIC PYRIDINONES
-
Paragraph 0366, (2015/11/02)
This application relates to polycyclic compounds with a pyridinone or pyridinone derivative core including, substituted pyridinones, 5,6- and 6,6- bicyclic heterocycles and substituted pyridine-thiones. This application also discloses methods of preparing these polycyclic compounds, pharmaceutical compositions and medicaments comprising said compounds and methods to treat, prevent or diagnose diseases, disorders or conditions associated with fibrosis.
ANTI-FIBROTIC PYRIDINONES
-
Paragraph 0619-0620, (2014/04/17)
Disclosed are pyridinone compounds, method for preparing these compounds, and methods for treating fibrotic disorders.
Rh(III)-catalyzed cascade oxidative olefination/cyclization of picolinamides and alkenes via C-H activation
Cai, Shangjun,Chen, Chao,Shao, Peng,Xi, Chanjuan
supporting information, p. 3142 - 3145 (2014/06/23)
Rh(III)-catalyzed cascade oxidative alkenylation/cyclization of picolinamides and alkenes to furnish pyrido pyrrolone derivatives is described, in which three C-H bonds and one N-H bond broke, while one C-C bond and one C-N bond formed. The reaction proceeded with high yield and high regioselectivity and stereoselectivity. Moreover, copper acetate can also be used in catalytic amounts with O2 serving as the terminal oxidant.
Copper-mediated hydroxylation of arenes and heteroarenes directed by a removable bidentate auxiliary
Li, Xin,Liu, Yan-Hua,Gu, Wen-Jia,Li, Bo,Chen, Fa-Jie,Shi, Bing-Feng
supporting information, p. 3904 - 3907 (2014/08/18)
A copper-mediated C-H hydroxylation of arenes and heteroarenes using our newly developed PIP directing group has been developed. This procedure is scalable and compatible with a wide range of functional groups and heteroarenes, providing an operationally simple protocol for the synthesis of o-hydroxybenzamides. The hydroxylation of nicotinamides gave 4-oxo-1,4-dihydropyridine-3-carboxamides selectively. Preliminary mechanistic studies implicate that a basic ligand-enabled, irreversible, rate-determining CMD step is most likely involved in this process.
OXADIAZOLE INHIBITORS OF LEUKOTRIENE PRODUCTION
-
Page/Page column 127, (2012/03/26)
The present invention relates to compound of formula (I) and pharmaceutically acceptable salt thereof, wherein R1-R5 are as defined herein. The invention also relates to pharmaceutical compositions comprising these compounds, methods of using these compounds in the treatment of various diseases and disorders, processes for preparing these compounds and intermediates useful in these processes.
Pd0/PR3-catalyzed arylation of nicotinic and isonicotinic acid derivatives
Wasa, Masayuki,Worrell, Brady T.,Yu, Jin-Quan
supporting information; experimental part, p. 1275 - 1277 (2010/05/02)
(Chemical Eqation Presented) Good for your health: Intermolecular C-H functionalization of pyridine rings at the 3- and 4-positions is described using a Pd0/PR3/ArBr catalytic system. This reaction provides a powerful method for the preparation of structurally diverse nicotinic and isonicotinic acids that are of great importance in drug discovery.
Novel Derivatives
-
Page/Page column 19, (2010/02/17)
The present invention relates to novel piperazine derivatives; to processes for their preparation; to pharmaceutical compositions containing the derivatives; and to the use of the derivatives in therapy to treat diseases for which blocking the Cav2.2 calcium channels is beneficial.