358780-14-0Relevant articles and documents
PROCESS FOR THE MANUFACTURE OF 2-SUBSTITUTED-5-(1-METHYLTHIO)ALKYLPYRIDINES
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, (2017/12/18)
Process for the manufacture of 2-substituted-5-(1-methylthio)alkylpyridines and a process for the manufacture of agriculturally or pharmaceutically active substances comprising the process for the manufacture of 2-substituted-5-(1- methylthio)alkylpyridines.
NOVEL GPR119 AGONIST COMPOUNDS
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, (2017/10/26)
The present invention relates to novel compounds of formula (I), process for preparation of the same and composition comprising these compounds.
Direct Aldehyde C-H Arylation and Alkylation via the Combination of Nickel, Hydrogen Atom Transfer, and Photoredox Catalysis
Zhang, Xiaheng,MacMillan, David W. C.
supporting information, p. 11353 - 11356 (2017/08/30)
A mechanism that enables direct aldehyde C-H functionalization has been achieved via the synergistic merger of photoredox, nickel, and hydrogen atom transfer catalysis. This mild, operationally simple protocol transforms a wide variety of commercially available aldehydes, along with aryl or alkyl bromides, into the corresponding ketones in excellent yield. This C-H abstraction coupling technology has been successfully applied to the expedient synthesis of the medicinal agent haloperidol.
Asymmetric Biocatalytic Synthesis of Fluorinated Pyridines through Transesterification or Transamination: Computational Insights into the Reactivity of Transaminases
López-Iglesias, María,González-Martínez, Daniel,Rodríguez-Mata, María,Gotor, Vicente,Busto, Eduardo,Kroutil, Wolfgang,Gotor-Fernández, Vicente
, p. 279 - 291 (2017/02/05)
The synthesis of a family of pyridines bearing a fluorinated substituent on the aromatic ring has been carried out through two independent and highly stereoselective chemoenzymatic strategies. Short chemical synthetic routes toward fluorinated racemic amines and prochiral ketones have been developed, which served as substrates to explore the suitability of lipases and transaminases in asymmetric biotransformations. The lipase-catalyzed kinetic resolution via acylation of racemic amines proceeded smoothly giving conversions close to 50% and excellent enantioselectivities. Alternatively, the biotransamination of the corresponding prochiral ketones was investigated giving access to both optically pure amine enantiomers using transaminases with complementary selectivity. High to quantitative conversion values were achieved, which allowed the isolation of the amines in moderate to high yields (40–88%). A deeper understanding of the latter process was enabled by performing theoretical calculations on thermodynamic and mechanistic aspects. Calculations showed that the biotransamination reactions are highly favoured by the presence of fluorine atoms and the pyridine ring. (Figure presented.).
Trifluoromethylation of (hetero)aryl iodides and bromides with copper(i) chlorodifluoroacetate complexes
Lin, Xiaoxi,Li, Zhengyu,Han, Xiaoyan,Weng, Zhiqiang
, p. 75465 - 75469 (2016/08/24)
A new copper-mediated trifluoromethylation reaction using copper(i) chlorodifluoroacetate complexes as reagents is reported. The complex [L2Cu][O2CCF2Cl] (L = bpy, dmbpy, phen) reacted with (hetero)aryl iodides and bromides in the presence of CsF in DMF at 75 °C to afford the trifluoromethylarenes in good to excellent yields. High compatibility with various chemical functions or (hetero)cycles was also observed in the reaction. A reaction mechanism involving a difluorocarbene intermediate, along with a subsequent formation of a -CF3 anion was proposed.
1,3-THIAZOL-2-YL SUBSTITUTED BENZAMIDES
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Page/Page column 379; 380, (2016/07/05)
The present invention relates to 1,3-thiazol-2-yl substituted benzamide compounds of general formula (I) as described and defined herein, to pharmaceutical compositions and combinations comprising said compounds and to the use of said compounds for manufacturing a pharmaceutical composition for the treatment or prophylaxis of a disease, in particular of neurogenic disorder, as a sole agent or in combination with other active ingredients.
METABOTROPIC GLUTAMATE RECEPTOR NEGATIVE ALLOSTERIC MODULATORS (NAMS) AND USES THEREOF
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Paragraph 00376, (2016/01/01)
Provided herein are small molecule active metabotropic glutamate subtype-2 and -3 receptor negative allosteric modulators (NAMs), compositions comprising the compounds, and methods of using the compounds and compositions.
SUBSTITUTED PYRIMIDINE COMPOUNDS AS mPGES-1 INHIBITORS
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Page/Page column 45, (2015/05/06)
The present disclosure is directed to substituted pyrimidine compounds of formula (I), and pharmaceutically acceptable salts thereof, as mPGES-1 inhibitors. These compounds are inhibitors of the microsomal prostaglandin E synthase-1 (mPGES-1) enzyme and a
Novel Imidazole Derivatives Useful for the Treatment of Arthritis
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, (2012/12/13)
The present invention provides compounds of the formula below: where A, X and R1-R6 are as described herein, a pharmaceutical salt thereof, and a pharmaceutical composition containing this compound; methods of treating pain associated with osteoarthritis using one of the compounds or a pharmaceutically acceptable salt thereof, and processes for preparing the compounds.
Synthesis of novel tetrahydroisoquinoline bronchodilators
Dalence-Guzmán, Maria F.,Toftered, J?rgen,Oltner, Viveca Thornqvist,Wensbo, David,Johansson, Martin H.
scheme or table, p. 4999 - 5003 (2010/10/05)
The synthesis and bronchorelaxing effects of a series of novel tetrahydroisoquinoline amides are described. The compounds were evaluated for their ability to relax LTD4 contracted isolated human small airways ex-vivo. Several compounds demonstrated highly
