- Examination of a Series of Ir and Rh PXL Pincer Complexes as (Pre)catalysts for Aromatic C-H Borylation
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This work follows a previously published study of high-turnover aromatic C-H borylation by Ir complexes supported by POCOP-type ligands incorporating-PiPr2 side donors (L1-L3) using HBpin in the presence of olefins. A variety of pincer-supported Ir and Rh
- Hung, Ming-Uei,Press, Loren P.,Bhuvanesh, Nattamai,Ozerov, Oleg V.
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Read Online
- Novel 1,3,5-triazinyl aminobenzenesulfonamides incorporating aminoalcohol, aminochalcone and aminostilbene structural motifs as potent anti-vre agents, and carbonic anhydrases i, ii, vii, ix, and xii inhibitors
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A series of 1,3,5-triazinyl aminobenzenesulfonamides substituted by aminoalcohol, ami-nostilbene, and aminochalcone structural motifs was synthesized as potential human carbonic an-hydrase (hCA) inhibitors. The compounds were evaluated on their inhibition
- Angeli, Andrea,Brázdová, Marie,Cs?llei, Jozef,Garaj, Vladimír,Havránková, Eva,Jampílek, Josef,Kemka, Miroslav,Mascaretti, ?árka,Moty?ka, Jozef,Soldánová, Zuzana,Supuran, Claudiu T.
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- Pyrrolopyrazole derivative, preparation method and medical application thereof
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The invention relates to pyrrolopyrazole derivative, a preparation method and application thereof in medicines. Specifically, the invention relates to a new pyrrolopyrazole derivative as shown in a general formula (I), a preparation method and application of the pyrrolopyrazole derivative or a pharmaceutical composition containing the pyrrolopyrazole derivative as a therapeutic agent, particularlyas a gastric acid secretion inhibitor and potassium-competitive acid blockers (P-CABs) in biological medicines. Specifically, the substituents (R1, R2, R3 and R4) in the general formula (I) are the same as the definitions in the specification.
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Paragraph 0090-0091
(2021/02/24)
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- Pyrrolopyrazole derivatives and preparation method thereof, and application of pyrrolopyrazole derivatives in medicines
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The invention relates to pyrrolopyrazole derivatives and a preparation method thereof, and application of the pyrrolopyrazole derivatives in medicines. Specifically, the invention relates to novel pyrrolopyrazole derivatives as shown in a general formula (I) in the specification, the preparation method of the pyrrolopyrazole derivatives and application of the pyrrolopyrazole derivatives or pharmaceutical compositions containing the pyrrolopyrazole derivatives as therapeutic agents, particularly as gastric acid secretion inhibitors and potassium ion competitive acid blockers P-CABs) in biological medicines. All the substituents (R1, R2, R3, R4 and R5) and a group (X) in the general formula (I) are as defined in the specification.
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Paragraph 0129-0130
(2021/03/13)
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- Continuous Flow Preparation of (Hetero)benzylic Lithiums via Iodine-Lithium Exchange Reaction under Barbier Conditions
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Herein we report the generation of benzylic lithiums via an iodine-lithium exchange reaction on benzylic iodides performed in continuous flow using tBuLi as the exchange reagent. The resulting benzylic lithium species are trapped in situ by carbonyl electrophiles under Barbier conditions, resulting in benzylic secondary and tertiary alcohols. This flow procedure further allows the generation of highly reactive heterobenzylic lithium compounds, which are difficult to generate under batch conditions. A general scale-up was possible without further optimization.
- Weidmann, Niels,Harenberg, Johannes H.,Knochel, Paul
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p. 5895 - 5899
(2020/08/12)
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- A General Catalytic Method for Highly Cost- and Atom-Efficient Nucleophilic Substitutions
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A general formamide-catalyzed protocol for the efficient transformation of alcohols into alkyl chlorides, which is promoted by substoichiometric amounts (down to 34 mol %) of inexpensive trichlorotriazine (TCT), is introduced. This is the first example of a TCT-mediated dihydroxychlorination of an OH-containing substrate (e.g., alcohols and carboxylic acids) in which all three chlorine atoms of TCT are transferred to the starting material. The consequently enhanced atom economy facilitates a significantly improved waste balance (E-factors down to 4), cost efficiency, and scalability (>50 g). Furthermore, the current procedure is distinguished by high levels of functional-group compatibility and stereoselectivity, as only weakly acidic cyanuric acid is released as exclusive byproduct. Finally, a one-pot protocol for the preparation of amines, azides, ethers, and sulfides enabled the synthesis of the drug rivastigmine with twofold SN2 inversion, which demonstrates the high practical value of the presented method.
- Huy, Peter H.,Filbrich, Isabel
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supporting information
p. 7410 - 7416
(2018/04/30)
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- DBN hexafluorophosphate salts as convenient sulfonylating and phosphonylating agents
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Air-stable N-sulfonyl and N-phosphonyl DBN hexafluorophosphate salts have been synthesised under mild conditions as sulfonylating and phosphonylating agents. These salts are highly efficient in the sulfonylation and phosphonylation of a range of N- and O-nucleophiles to generate sulfonamides, sulfonate esters, phosphoramidates and phosphonate esters in good yields.
- Jones, Caroline S.,Bull, Steven D.,Williams, Jonathan M. J.
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supporting information
p. 8452 - 8456
(2016/09/28)
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- Halogenation of primary alcohols using a tetraethylammonium halide/[Et 2NSF2]BF4 combination
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The halogenation of primary alcohols is presented. The use of a combination of tetraethylammonium halide and [Et2NSF2]BF4 (XtalFluor-E) allows for chlorination and bromination reactions to proceed efficiently (up to 92% yield) with a wide range of alcohols. Iodination reactions are also possible albeit in lower yields.
- Pouliot, Marie-France,Mahe, Olivier,Hamel, Jean-Denys,Desroches, Justine,Paquin, Jean-Francois
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supporting information
p. 5428 - 5431,4
(2020/10/15)
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- Synthesis and biological evaluation of nitric oxide-donating thalidomide analogues as anticancer agents
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In search of more potent anticancer agents, 15 nitric oxide (NO)-donating thalidomide analogues, 6a, 6b, 8a-8e, and 13a-13h, were designed and synthesized. Cytotoxicity of these compounds was evaluated in vitro against three human tumor cell lines (HepG2, A549, and PC-3). The results indicated that 13a-13d exhibited notable anticancer activities comparable to or stronger than that of 5-fluorouracil (5-FU). Structure-activity relationships were also discussed, based on the experimental data obtained. Generally, the cytotoxic activity of target compounds is closely related to the type of NO donors, and the length of the spacers connecting to NO donors also appears important for the bioactivities.
- Wang, Tao,Zhang, Yi-Hua,Kong, Xiang-Wen,Lai, Yi-Sheng,Ji, Hui,Chen, Yan-Ping,Peng, Si-Xun
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experimental part
p. 466 - 474
(2010/04/23)
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- New NO-releasing pharmacodynamic hybrids of losartan and its active metabolite: Design, synthesis, and biopharmacological properties
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In a preliminary work, we reported two NO-sartans, possessing the characteristics of an AT1 antagonist and a "slow NO donor", obtained by adding NO-donor side chains to losartan 1. The NO release from an NO-sartan should be modulated in order to strengthen the antihypertensive activity of the native drug and to ensure additional effects, such as the antiplatelet and anti-ischemic ones. To obtain a collection of proto-typical NO-sartans, showing different rates of NO release, new NO-donor moieties have been linked to 1 or its active metabolite 2 (EXP 3174). Almost all the synthesized compounds exhibited both AT1-antagonist and NO-mediated vasorelaxing properties, with a wide range of NO-releasing rates. Further pharmacological investigation on compound 4a showed that it possessed antihypertensive and cardiac antihypertrophic effects similar to those of the reference AT1-blocking or ACE-inhibiting drugs. Furthermore, the additional anti-ischemic cardio-protective properties and antiplatelet effects of 4a have been preliminarily investigated.
- Breschi, Maria C.,Calderone, Vincenzo,Digiacomo, Maria,Macchia, Marco,Martelli, Alma,Martinotti, Enrica,Minutolo, Filippo,Rapposelli, Simona,Rossello, Armando,Testai, Lara,Balsamo, Aldo
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p. 2628 - 2639
(2007/10/03)
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- INDENE DERIVATIVES AND PROCESS FOR THE PREPARATION THEREOF
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The inventive indene derivatives of formula (I) are capable of selectively modulating the activities of peroxisome proliferator activated receptors (PPARs), causing no adverse side effects, and thus, they are useful for the treatment and prevention of disorders modulated by PPARs, i.e., metabolic syndromes such as diabetes, obesity, arteriosclerosis, hyperlipidemia, hyperinsulinism and hypertension, inflammatory diseases such as osteoporosis, liver cirrhosis and asthma, and cancer.
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Page/Page column 36
(2010/02/14)
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- Reduction of carbonyl compounds promoted by silicon hydrides under the influence of trimethylsilyl-based reagents
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The synthetic utility of hydrosilanes under the influence of trimethylsilyl-based reagents as new reducing systems is described. 1,1,3,3-Tetramethyldisiloxane (TMDS) reagent in combination with iodotrimethylsilane or bromotrimethylsilane produces alkyl halides from aldehydes in good to excellent yields.Polymethylhydrosiloxane (PMS) in the presence of iodotrimethylsilane also produces benzyl iodides in excellent yields.On the contrary, PMS reagent was found unsuitable for the synthesis of benzyl bromides.Similary, TMDS reagent in combination with trimethylsilyl triflate produces symmetrical ethers from aldehydes without concomitant formation of competitive products.Under similar conditions, PMS reagent failed to provide the expected symmetrical ethers and Friedel-Crafts products were formed.Reduction of quinones to hydroquinones is also described.
- Aizpurua, Jesus M.,Lecea, Begona,Palomo, Claudio
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p. 2342 - 2347
(2007/10/02)
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- Synthetic Application of Lithiation Reaction: Part XVIII - Synthesis of (+/-)-3,4-Dihydro-3-phenylisocoumarin and Aglycone of (+/-)-Dihydrohomalicine
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N-Methylbenzamide on lithiation with n-butyllithium followed by reaction with N-methylformanilide gives compound (1), which on hydrolysis with dil.HCl furnishes 2-formylbenzoic acid (2).This acid on reaction with benzylidenetriphenylphosphorane gives stil
- Narasimhan, N. S.,Mali, R. S.,Kulkarni, B. K.
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p. 850 - 852
(2007/10/02)
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