61844-32-4Relevant academic research and scientific papers
Dopamine D2 receptor selective agonist and application thereof
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, (2020/12/29)
The invention relates to a dopamine D2 receptor selective agonist and application thereof. Specifically, the invention discloses an agonist with selectivity to DRD2 and discloses a potential application value of the agonist in disease treatment. The invention discloses an agonist with DRD2 selectivity for the first time, and the specific targeting DRD2 of the agonist can play a role in treating low dopamine related diseases such as Parkinson's disease, attention deficit hyperactivity disorder, pituitary adenoma, hyperprolactinemia, hyperactivity leg syndrome, negative schizophrenia and the like while side effects are reduced to the maximum extent.
Selective hydrogenation of conjugated unsaturated ketones containing a hydroxyaryl substituent in the β-position
Kovalenko,Pratsko
, p. 24 - 28 (2017/03/16)
A high selectivity was achieved in the Ni2B-catalyzed hydrogenation of α,β-unsaturated ketones containing a hydroxyaryl (phenolic) substituent in the β-position. The developed hydrogenation procedure was used to synthesize natural compounds of the phenylpropane series and their structural analogs.
Decarboxylative Csp3-Csp3 coupling for benzylation of unstable ketone enolates: Synthesis of: P -(acylethyl)phenols
Wang, Sasa,Chen, Xinzheng,Ao, Qiaoqiao,Wang, Huifei,Zhai, Hongbin
, p. 9454 - 9457 (2016/07/29)
A new decarboxylative Csp3-Csp3 coupling approach for the benzylation of ketone enolates has been developed. A variety of raspberry ketone derivatives were conveniently synthesized in good to excellent yields under mild conditions. A crossover reaction shed light on the mechanism of this tandem reaction.
Michael additions of highly basic enolates to ortho -quinone methides
Lewis, Robert S.,Garza, Christopher J.,Dang, Ann T.,Pedro, Te Kie A.,Chain, William J.
, p. 2278 - 2281 (2015/05/13)
A protocol by which ketone or ester enolates and ortho-quinone methides (o-QMs) are generated in situ in a single reaction flask from silylated precursors under the action of anhydrous fluoride is reported. The reaction partners are joined to give a variety of β-(2-hydroxyphenyl)-carbonyl compounds in 32-94% yield in a single laboratory operation. The intermediacy of o-QMs is supported by control experiments utilizing enolate precursors and conventional alkyl halides as competitive alkylating agents and the isolation of 1,5-dicarbonyl products resulting from conjugate additions that do not restore the aromatic system.
Pd(II)-catalyzed asymmetric Wacker-type cyclization for the preparation of 2-vinylchroman derivatives with biphenyl tetraoxazoline ligands
Liu, Qingchuan,Wen, Ke,Zhang, Zhenfeng,Wu, Zhengxing,Zhang, Yong Jian,Zhang, Wanbin
, p. 5209 - 5215 (2012/08/08)
This article describes an efficient method for the preparation of chiral chroman derivatives by the Pd(II)-catalyzed asymmetric Wacker-type cyclization using a chelation-induced axially chiral tetraoxazoline ligand. Under the optimized conditions, up to 80% yield and up to 92% ee were obtained. This is the first example to utilize o-trisubstituted 3-butenylphenols as substrates in such transformation.
HETEROCYCLIC COMPOUNDS USEFUL AS ANABOLIC AGENTS FOR LIVESTOCK ANIMALS
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, (2008/06/13)
Compounds of formula (I) and pharmaceutically acceptable salts thereof are agonists at the beta-2 adrenoceptor. They are useful as feed additives for livestock animals.
Enantioselective synthesis of chromanes by iridium-catalyzed asymmetric hydrogenation of 4H-chromenes
Valla, Carine,Baeza, Alejandro,Menges, Frederik,Pfaltz, Andreas
experimental part, p. 3167 - 3171 (2009/06/17)
Iridium complexes of chiral oxazoline-based P,N-ligands proved to be efficient catalysts for the enantioselective hydrogenation of 2-aryl- and 2-alkyl-4H-chromenes. The best results were obtained with a ligand derived from threonine (ThrePHOX), which induced ee values of 95% to >99% in the hydrogenation of 2-methyl-, 2-cyclohexyl- and various 2-aryl-substituted chromenes. Georg Thieme Verlag Stuttgart.
Benzoyl 2-methyl indoles as selective PPARγ modulators
Acton III, John J.,Black, Regina M.,Jones, A. Brian,Moller, David E.,Colwell, Lawrence,Doebber, Thomas W.,MacNaul, Karen L.,Berger, Joel,Wood, Harold B.
, p. 357 - 362 (2007/10/03)
A series of selective PPARγ modulators (SPPARγMs) and their development from hPPARγ active screening leads 1 and 2 is described. SPPARγM 24 displayed robust anti-diabetic activity with an improved therapeutic window in comparison to a PPARγ full agonist in a rodent efficacy model. Routine screening for human PPAR ligands yielded compounds 1 and 2, both of which were sub-micromolar hPPARγ agonists. Synthetic modifications of these leads led to a series of potent substituted 3-benzyl-2-methyl indoles, a subset of which were noted to be selective PPARγ modulators (SPPARγMs). SPPARγM 24 displayed robust anti-diabetic activity with an improved therapeutic window in comparison to a PPARγ full agonist in a rodent efficacy model.
Ionic hydrogenation of α,β-unsaturated ketones with cyclohexane in the presence of aluminum halides
Koltunov,Repinskaya,Borodkin
, p. 1534 - 1541 (2007/10/03)
4-Methyl-3-penten-2-one, 3-hepten-2-one, 3-methyl-1-phenyl-2-buten-1-one, 4-(2,4-dichlorophenyl)-, 4-(4-hydroxyphenyl)-, 4-(4-methoxyphenyl)-, 4-(2-hydroxyphenyl)-, and 4-(4-dimethylaminophenyl)-3-buten-2-ones, and 3-(4-methoxyphenyl)-1-phenyl-2-propenone react with cyclohexane in the presence of excess aluminum chloride or aluminum bromide in CH2Cl2 or CH2Br2, respectively, at room temperature to form the corresponding saturated ketones in high yields. Using 4-phenyl-and 4-(4-methoxyphenyl)-3-buten-2-ones as examples, it was shown that the reaction pattern does not change in going from the Lewis acids AlCl3, and AlBr3 to proton-donor acid system CF3SO3H-SbF5. The reactive intermediates are likely to be C-protonated complexes of α,β-unsaturated ketones with aluminum halides or their O,C-diprotonated analogs.
