- 2-(2,2-DIARYLETHYL)-CYCLIC AMINE DERIVATIVE OR SALT, SYNTHESIS THEREOF, AND APPLICATION AND COMPOSITION THEREOF
-
The disclosure relates to a 2-(2,2-diarylethyl)-cyclic amine derivative or salt, a synthesis method, an application and a composition thereof. Biological activity test shows that this kind of 2-(2,2-diarylethyl)-cyclic amine derivative has good M-receptor antagonistic activity; and can be used as an active component of drugs for the treatment of the diseases mediated or regulated by muscarinic receptors, such as asthma, chronic obstructive pulmonary disease (COPD), overactive bladder (OAB), bronchospasm with chronic obstructive pulmonary disease, visceral spasm, irritable bowel syndrome, Parkinson's disease, depression or anxiety, schizophrenia and related mental diseases.
- -
-
Paragraph 0238-0239; 0364-0365
(2021/05/28)
-
- Eco-friendly organocatalyst- And reagent-controlled selective construction of diverse and multifunctionalized 2-hydroxybenzophenone frameworks for potent UV-A/B filters by cascade benzannulation
-
The organocatalyst- and reagent-controlled highly selective synthesis of diversely functionalized novel 2-hydroxybenzophenone frameworks, such as 2-hydroxy-3′-formylbenzophenones, 7-(2′-hydroxybenzoyl)-2-naphthaldehydes, and 2-hydroxybenzophenones, under green conditions, for the development of potent UV-A/B filters is described. The organocatalyzed benzannulation reactions proceed individually via [3 + 3] cycloaddition for the synthesis of 2-hydroxy-3′-formylbenzophenones and [4 + 2] cycloaddition for 2-hydroxybenzophenones. With this methodology, an unprecedented double benzannulation allows one-pot construction of diverse 7-(2′-hydroxybenzoyl)-2-naphthaldehydes via [3 + 3 + 4] cycloaddition. This protocol features a broad substrate scope, high functional-group tolerance, and operational simplicity in an environmentally benign green solvent. The synthesized compounds are successfully utilized for further transformations and well characterized as potent UV-A/B filters.
- Akhtar, Muhammad Saeed,Inductivo Tamargo, Ramuel John,Kim, Sung Hong,Lee, Yong Rok,Thombal, Raju S.,Yang, Won-Guen
-
supporting information
p. 4523 - 4531
(2020/08/10)
-
- Diaryl vinyl cyclic amine derivatives and preparation method thereof
-
The invention provides diaryl vinyl cyclic amine derivatives and a preparation method thereof. The aryl substituted groups of the diaryl vinyl cyclic amine derivatives have a hydroxyl or hydroxy derivative functional groups in the ortho positions of vinyl groups. The bioactivity test shows that the compounds have anticholinergic activity, and the ortho-hydroxy groups can significantly enhance theantagonistic activity; the compounds can be used as active pharmaceutical ingredients for treating asthma, chronic obstructive pulmonary disease (COPD), rhinorrhea caused by allergic rhinitis and cold, urinary incontinence, Parkinson's disease, and the like.
- -
-
Paragraph 0144; 0145; 0330-0334
(2018/09/08)
-
- Operationally Simple and Selective One-Pot Synthesis of Hydroxyphenones: A Facile Access to SNARF Dyes
-
High selectivity is observed during a Friedel-Crafts acylation/demethylation cascade. In contrast to this cascade, oxygen-containing acylating reagents do not undergo the demethylation step. By the methodology elaborated here, an access is provided to important intermediates for the total synthesis of seminaphthorhodafluor (SNARF) dyes.
- Richter, Celin,Ernsting, Nikolaus P.,Mahrwald, Rainer
-
p. 1217 - 1225
(2016/05/11)
-
- Hypervalent iodine in synthesis 59: Application of polymeric diaryliodonium salts as aryl transfer reagents in SPOS
-
Polymeric diaryliodonium salts were employed as aryl transfer reagents in the Pd(II) catalyzed cross-coupling reaction with salicylaldehydes, and could be regenerated and recycled for the same reactions.
- Chen,Chen
-
p. 1175 - 1177
(2007/10/03)
-
- Hypervalent iodine in synthesis XXXIV: Palladium-catalyzed coupling reaction of o-hydroxyarylaldehydes with hypervalent iodonium salts via cleavage of the aldehyde C-H bond
-
A novel way of preparation for o-hydroxyarylketones with mild conditions and good yields by palladium-catalyzed coupling reaction of o- hydroxyarylaldehydes with hypervalent iodonium salts via the cleavage of the aldehyde C-H bond has been reported.
- Xia, Min,Chen, ZhenChu
-
p. 531 - 536
(2007/10/03)
-
- Cyclodeshydratation d'aryloxy-2 diaryl-1,2 ethanones en diaryl-2,3 benzofurannes. Influence de la substitution sur la competition entre deux chemins reactionnels
-
Many of the methods for synthesizing derivatives of 2,3-diaryl benzofurans imply cyclodehydration of 1,2-diaryl 2-aryloxyethanones, leading often to a mixture of two isomers which differ by the presence of the aryl substituent at positions C-2 or C-3 of benzofuran.This isomerisation is explained by a competition between two possible mechanisms.Either a direct electrophilic substitution or the intermediate formation of an α-acylcarbenium ion.This study deals with the competition as determined by the substitution of aryl groups in the initial substrate.Each 2,3-diarylbenzofuran was synthesized previously using an unambiguous method.
- Montfort, Bernard,Laude, Bernard,Vebrel, Joel,Cerutti, Ernest
-
p. 848 - 854
(2007/10/02)
-