- Growth Factor Receptor antagonists. Preparation method and application thereof
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The invention relates to a small molecule antagonist for transforming growth factor β receptors, a method for preparing the small molecule antagonist, and application of the small molecule antagonist in preparation of drugs. The small molecule antagonist for transforming the growth factor β receptor has the application of treating and/or preventing various diseases mediated by ALK5, and has great clinical application potential.
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Paragraph 0125-0130
(2021/11/10)
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- Nickel-catalyzed carboxylation of aryl and heteroaryl fluorosulfates using carbon dioxide
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The development of efficient and practical methods to construct carboxylic acids using CO2 as a C1 synthon is of great importance. Nickel-catalyzed carboxylation of aryl fluorosulfates and heteroaryl fluorosulfates with CO2 is described, affording arene carboxylic acids with good to excellent yields under mild conditions. In addition, a one-pot phenol fluorosulfation/carboxylation is developed.
- Ma, Cong,Zhao, Chuan-Qi,Xu, Xue-Tao,Li, Zhao-Ming,Wang, Xiang-Yang,Zhang, Kun,Mei, Tian-Sheng
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p. 2464 - 2467
(2019/04/10)
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- Polysubstituted pyridine medical intermediate and synthetic method thereof
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The invention belongs to the field of medicine intermediate technology, and specifically relates to a polysubstituted pyridine medical intermediate and a synthetic method thereof. The polysubstituted pyridine medical intermediate is a key intermediate in pharmaceutical synthesis, and has a huge market potential. The synthetic method has simple synthetic route, simple and easily available staring material, and has great meaning in synthesis of pyridine intermediate, development of pyridine medicament and research and development of novel medicament, and the product is cheap.
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Paragraph 0047; 0048; 0049; 0050
(2016/10/08)
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- Preparation of 4,7-diphenyl-1,10-phenanthroline-2,9-dicarboxylic acid catalyzed by iron(III)porphyrins with (diacetoxyiodo)benzene
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Using iron(III)porphyrins in combination with (diacetoxyiodo)benzene allows for the conversion of 2,9-bis(bromomethyl)-4,7-diphenyl-1,10-phenanthroline into 4,7-diphenyl-1,10-phenanthroline-2,9-dicarboxylic acid. This method provides a cost-effective and environmentally-friendly oxidation procedure using less toxic PhI(OAc)2 and biologically relevant iron(III)porphyrins. The catalytic activity of five kinds of iron-metallated functional porphyrins were investigated using different oxidants, including air, H2O 2, PhI(OAc)2, PhIO and NaClO. Our results showed that the use of T(p-NO2)PPFeCl with PhI(OAc)2 as the oxidant in the presence of water displays remarkable activity for the desired oxidation reaction. The generality of this method was examined by synthesizing the carboxylic acids of pyridines and quinolines.
- Zhong, Qi-Di,Xue, Yun-Zhou,Yan, Hong,Song, Xiu-Qing,Zhong, Ru-Gang
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body text
p. 5532 - 5535
(2010/12/20)
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- Process for producing heterocyclic aldehyde
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The present invention provides a process for preparing a heterocyclic aldehyde by oxidizing a heterocyclic alcohol with high selectivity and high yield. Specifically, the heterocyclic aldehyde is prepared by reacting a heterocyclic compound having at least one hydroxymethyl group bonded to a carbon atom of a heterocyclic ring with a hypohalogenous acid salt in the presence of a base to oxidize the hydroxymethyl group, wherein reaction is conducted in the co-presence of a 2,2,6,6-tetramethylpiperidine-1-oxyl derivative having at least two 2,2,6,6-tetramethylpiperidine-1-oxyl-4-yl groups.
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Page/Page column 11
(2008/06/13)
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- ARYL SULFONAMIDES
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The present invention relates to compounds that modulate various chemokine receptors. These compounds are useful for treating inflammatory and immune diseases.
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Page/Page column 178
(2010/02/14)
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- A long-range chiral relay via tertiary amide group in asymmetric catalysis: new amino acid-derived N,P-ligands for copper-catalysed conjugate addition.
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New N,P-ligands 4-6, derived from valinol and prolinol, respectively, have been developed for the asymmetric, copper(I)-catalysed conjugate addition of diethylzinc to unsaturated ketones; the tertiary amide group has been shown to effectively relay the chiral information from the ligand backbone to the active centre.
- Malkov, Andrei V,Hand, John B,Kocovsky, Pavel
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p. 1948 - 1949
(2007/10/03)
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- Catechol 2,3-Dioxygenase-catalyzed Synthesis of Picolinic Acids from Catechols
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Various picolinic acid derivatives were synthesized from ammonia and hydroxymuconic semialdehyde derivatives that were oxidatively prepared from various catechols by the action of Pseudomonas catechol 2,3-dioxygenase (C23O, metapyrocatechase).
- Asano, Yasuhisa,Yamamoto, Yasushi,Yamada, Hideaki
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p. 2054 - 2056
(2007/10/02)
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