- ALPHAvBETA1 INTEGRIN ANTAGONISTS
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The present disclosure provides pharmaceutical agents, including those of the formula: (I) wherein the variables are defined herein. Also provided are pharmaceutical compositions, kits and articles of manufacture comprising such pharmaceutical agents. Methods of using the pharmaceutical agents are also provided. The compounds may be used for the inhibition or antagonism of integrins ανβ1 and/or α5β1. In some embodiments, the compounds provided herein exhibit reduced inhibitory or antagonistic activity of integrins ανβ3, ανβ5, ανβ6, ανβ8, and/or αIIbβ3.
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Paragraph 0171; 0251
(2020/01/31)
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- Novel antioxidant and preparation method thereof
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The invention relates to a novel antioxidant and a preparation method thereof. The structural formula of the antioxidant is shown in img file = 'dest _ path _ image 001. TIF 'wi = '152 'he = '86 ', wherein R is an alkyl group CnH2n +1, and n is 0 to 22. A
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Paragraph 0016; 0017
(2017/08/28)
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- Palladium-Catalyzed, tert-Butyllithium-Mediated Dimerization of Aryl Halides and Its Application in the Atropselective Total Synthesis of Mastigophorene A
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A palladium-catalyzed direct synthesis of symmetric biaryl compounds from aryl halides in the presence of tBuLi is described. In situ lithium-halogen exchange generates the corresponding aryl lithium reagent, which undergoes a homocoupling reaction with a second molecule of the aryl halide in the presence of the palladium catalyst (1 mol %). The reaction takes place at room temperature, is fast (1 h), and affords the corresponding biaryl compounds in good to excellent yields. The application of the method is demonstrated in an efficient asymmetric total synthesis of mastigophorene A. The chiral biaryl axis is constructed with an atropselectivity of 9:1 owing to catalyst-induced remote point-to-axial chirality transfer. It takes two: A palladium-catalyzed direct homocoupling of aryl halides in the presence of tBuLi enabled the synthesis of even tetra-ortho-substituted symmetric biaryl compounds in high yield (see scheme). The method was applied to the asymmetric synthesis of mastigophorene A in just eight steps through straightforward enantioselective installation of the benzylic quaternary stereocenter and highly diastereoselective homocoupling.
- Buter, Jeffrey,Heijnen, Dorus,Vila, Carlos,Hornillos, Valentín,Otten, Edwin,Giannerini, Massimo,Minnaard, Adriaan J.,Feringa, Ben L.
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supporting information
p. 3620 - 3624
(2016/03/23)
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- Benzylic C-H trifluoromethylation of phenol derivatives
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Phenol derivatives were trifluoromethylated using copper/Togni reagent. In dimethylformamide, the benzylic C-H bond at the para position of the hydroxyl group was selectively substituted with a CF3 group. In contrast, aromatic C-H trifluorometh
- Egami, Hiromichi,Ide, Takafumi,Kawato, Yuji,Hamashima, Yoshitaka
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p. 16675 - 16678
(2015/11/25)
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- Encapsulation and release mechanisms in coordination polymer nanoparticles
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The interplay of guest encapsulation and release mechanisms in nanoscale metal-organic vehicles and its effect on the drug-delivery kinetics of these materials were investigated through a new multidisciplinary approach. Two rationally-designed molecular g
- Amorin-Ferre, Laura,Busque, Felix,Bourdelande, Jose Luis,Ruiz-Molina, Daniel,Hernando, Jordi,Novio, Fernando
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p. 17508 - 17516
(2014/01/06)
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- Self-assembly of alkylcatechols on HOPG investigated by scanning tunneling microscopy and molecular dynamics simulations
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Two alkylcatechols have been studied by means of STM at the liquid-solid interface. While for catechol 3 no molecular domains on the surface have been observed most likely due to the steric constraints imposed by the tert-butyl group, catechol 2 self-orga
- Saiz-Poseu, Javier,Alcon, Isaac,Alibes, Ramon,Busque, Felix,Faraudo, Jordi,Ruiz-Molina, Daniel
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experimental part
p. 264 - 271
(2012/03/08)
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- An efficient method for the synthesis of lignans
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An efficient approach for the synthesis of several types of lignans (dibenzylbutanediols, dibenzylbutanes, substituted tetrahydrofurans, aryldihydronaphthalenes, arylnaphthalenes, and aryltetralins) was developed. The regioselective oxidative coupling of ethyl ferulate was used as the key step.
- Wang, Qian,Yang, Yong,Li, Ying,Yu, Wei,Hou, Zi Jie
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p. 6107 - 6112
(2007/10/03)
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- Regioselective oxidative coupling approach to the synthesis of (±)-matairesinol and (±)-secoisolariciresinol
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An efficient method for the synthesis of (±)-matairesinol and (±)-secoisolariciresinol is presented. By using 5-(tert-butyl)ferulic acid as a precursor, a regioselective oxidative coupling step was realized, which gave the desired coupling product in much higher yield (91%) than the literature value (ca. 20%). Georg Thieme Verlag Stuttgart.
- Zhu, Fuqiang,Li, Wenling,Wang, Qian,Hou, Zijie
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p. 1780 - 1782
(2008/02/04)
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- Reactions of 1-Oxaspiroocta-5,7-dien-4-ones with Nucleophiles
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The 1-oxaspiroocta-5,7-dien-4-ones (6-spiroepoxy-2,4-cyclohexadienones) (7) on reaction with a number of carbon, nitrogen, oxygen and halogen nucleophiles produced a variety of interesting substitution and rearrangement products (8)-(19) in moderate yields.The products derived almost exclusively from initial attack of the nucleophile with either the secondary or quaternary carbon of the epoxy ring and these various modes of reaction of the spirocyclic system are discussed.The formation of ortho-substituted phenols from the 1-oxaspiroocta-5,7-dien-4-ones suggests that the latter structures may be regarded as polarity-reversed masked phenols.Tropolones, products of a possible ring-expansion reaction, were not observed in any of the reactions investigated.
- Cacioli, Paul,Reiss, James A.
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p. 2525 - 2535
(2007/10/02)
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