- Poly(vinyl ketone)s by controlled boron group transfer polymerization (BGTP)
-
(Figure Presented) Boron can do it! Readily prepared catecholboron enolates act as regulators in the controlled radical polymerization of alkyl and aryl vinyl ketones. Control is achieved by an unprecedented reversible radical boron group transfer (BGT) between enoyl radicals (see scheme). Polymers with M n-1 and a polydispersity index of 1.3 can be obtained by this process.
- Uehara, Kazuhiro,Wagner, Christine B.,Vogler, Thomas,Luftmann, Heinrich,Studer, Armido
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-
Read Online
- Acetyl nitrate mediated conversion of methyl ketones to diverse carboxylic acid derivatives
-
The development of a novel acetyl nitrate mediated oxidative conversion of methyl ketones to carboxylic acid derivatives is described. By analogy to the haloform reaction and supported by experimental and computational investigation we propose a mechanism for this transformation.
- Bernard, Josephine,Capilato, Joseph N.,Hoy, Erik P.,Mattiucci, Joseph,Pellegrinelli, Peter J.,Perez, Lark J.,Philippi, Shane,Schnorbus, Logan
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supporting information
p. 5298 - 5302
(2021/06/30)
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- NOVEL COMPOUNDS HAVING ANTI-INFLAMMATORY ACTIVITY AS P38 MAP KINASE INHIBITOR
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The present invention relates to novel compounds exhibiting anti-inflammatory activity. The compound of the present invention plays a critical role in the production of inflammatory prodrug (pro-inflammatory cytokines) and has an excellent inhibitory effect on p38 MAPK, which is known to cause inflammatory diseases, and thus can be used as a therapeutic agent for inflammatory diseases.
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-
Paragraph 0063-0064
(2021/09/14)
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- Rhoda-Electrocatalyzed Bimetallic C?H Oxygenation by Weak O-Coordination
-
Rhodium-electrocatalyzed arene C?H oxygenation by weakly O-coordinating amides and ketones have been established by bimetallic electrocatalysis. Likewise, diverse dihydrooxazinones were selectively accessed by the judicious choice of current, enabling twofold C?H functionalization. Detailed mechanistic studies by experiment, mass spectroscopy and cyclovoltammetric analysis provided support for an unprecedented electrooxidation-induced C?H activation by a bimetallic rhodium catalysis manifold.
- Tan, Xuefeng,Massignan, Leonardo,Hou, Xiaoyan,Frey, Johanna,Oliveira, Jo?o C. A.,Hussain, Masoom Nasiha,Ackermann, Lutz
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supporting information
p. 13264 - 13270
(2021/05/06)
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- Synthesis of various acylating agents directly from carboxylic acids
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A straightforward synthesis of acylating reagents such as Weinreb and MAP amides from aromatic, aliphatic carboxylic acids, and amino acids using PPh3/NBS combination is described. A chemo-selective modification of the carboxylic acid group into Weinreb amide in the presence of more reactive aldehydes and ketones is presented. All reactions were performed at ambient temperature under air using undried commercial grade solvent. Furthermore, the present methodology could be performed at a gram scale under inert-free reaction conditions. In addition, 7-azaindoline amide auxiliary (used for catalytic asymmetric aldol- and Mannich-type reactions), which behaves like Weinreb amide is also synthesized under similar reaction conditions.
- Pilathottathil, Fathima,Vineet Kumar, Doppalapudi,Kaliyamoorthy, Alagiri
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supporting information
p. 1622 - 1632
(2020/04/27)
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- Saturated Bioisosteres of ortho-Substituted Benzenes
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Saturated bioisosteres of ortho-disubstituted benzenes (bicyclo[2.1.1]hexanes) were synthesized, characterized and validated. These cores were incorporated into the bioactive compounds Valsartan, Boskalid and Fluxapyroxad instead of the benzene ring. The
- Denisenko, Aleksandr,Garbuz, Pavel,Mykhailiuk, Pavel K.,Shishkina, Svetlana V.,Voloshchuk, Nataliya M.
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supporting information
p. 20515 - 20521
(2020/08/21)
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- An α-Cyclopropanation of Carbonyl Derivatives by Oxidative Umpolung
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The reactivity of iodine(III) reagents towards nucleophiles is often associated with umpolung and cationic mechanisms. Herein, we report a general process converting a range of ketone derivatives into α-cyclopropanated ketones by oxidative umpolung. Mechanistic investigation and careful characterization of side products revealed that the reaction follows an unexpected pathway and suggests the intermediacy of non-classical carbocations.
- Bauer, Adriano,Di Mauro, Giovanni,Li, Jing,Maulide, Nuno
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p. 18208 - 18212
(2020/08/21)
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- Fluoro-Substituted Methyllithium Chemistry: External Quenching Method Using Flow Microreactors
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The external quenching method based on flow microreactors allows the generation and use of short-lived fluoro-substituted methyllithium reagents, such as fluoromethyllithium, fluoroiodomethyllithium, and fluoroiodostannylmethyllithium. Highly chemoselective reactions have been developed, opening new opportunities in the synthesis of fluorinated molecules using fluorinated organometallics.
- Colella, Marco,Degennaro, Leonardo,Higuma, Ryosuke,Ishikawa, Susumu,Luisi, Renzo,Nagaki, Aiichiro,Takahashi, Yusuke,Tota, Arianna
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supporting information
p. 10924 - 10928
(2020/05/08)
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- Iminyl Radicals by Reductive Cleavage of N-O Bond in Oxime Ether Promoted by SmI2: A Straightforward Synthesis of Five-Membered Cyclic Imines
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A new generation method of N-centered radicals from the reductive cleavage of the N-O bond in oxime ether promoted by SmI2 is reported for the first time. The in-situ-generated N-centered radicals underwent intramolecular cyclization to afford five-membered cyclic imines in two manners: N-centered radical addition and N-centered anion nucleophilic substitution. From a synthetic point of view, an efficient synthetic method of five-membered cyclic imines was developed. A mechanism of the transformation was proposed.
- Huang, Fei,Zhang, Songlin
-
supporting information
p. 7430 - 7434
(2019/10/11)
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- Broadly Applicable Ytterbium-Catalyzed Esterification, Hydrolysis, and Amidation of Imides
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An efficient, broadly applicable, operationally simple, and divergent process for the transformation of imides into a range of carboxylic acid derivatives under mild conditions is reported. By simply using catalytic amounts of ytterbium(III) triflate as a Lewis acid promoter in the presence of alcohols, water, amines, or N,O-dimethylhydroxylamine, a broad range of imides is smoothly and readily converted to the corresponding esters, carboxylic acids, amides, and Weinreb amides in good yields. This method notably enables an easy cleavage of oxazolidinone-based auxiliaries.
- Guissart, Céline,Barros, Andre,Rosa Barata, Luis,Evano, Gwilherm
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supporting information
p. 5098 - 5102
(2018/09/13)
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- DIHYDROPYRIDAZINONES SUBSTITUTED WITH PHENYLUREAS
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Compounds of formula (I) which are nicotinamide phosphoribosyltransferase (NAMPT) inhibitors and their use for the treatment of hyperproloferative diseases and/or disorders responsive to induction of cell death.
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Page/Page column 252
(2018/05/27)
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- PIPERIDINE COMPOUNDS AS PCSK9 INHIBITORS
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One aspect of the invention relates to a series of new PCSK9 inhibitor compounds comprising piperidine ring structures, including compounds of formula (I) and/or pharmaceutically acceptable salts thereof. Another aspect of the invention relates to methods of treating PCSK9 receptor related diseases comprising administration of one or more compounds of formula (I) or a pharmaceutically acceptable salt thereof.
- -
-
Paragraph 0099; 0100; 0101
(2018/11/21)
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- Design, synthesis, and biological evaluation of aryl N-methoxyamide derivatives as GPR119 agonists
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A series of N-methoxyamide derivatives was identified and evaluated as GPR119 agonists. Several N-methoxyamides with thienopyrimidine and pyridine scaffolds showed potent GPR119 agonistic activities. Among them, compound 9c displayed good in vitro activity and potency. Moreover, compound 9c lowered glucose excursion in mice in an oral glucose tolerance test and increased GLP-1 secretion in intestinal cells.
- Jang, Yoon Kyung,Lee, Kyu Myung,Jung, Kwan-Young,Kang, Seung Kyu,Pagire, Suvarna H.,Lee, Jun Mi,Pagire, Haushabhau S.,Kim, Kwang Rok,Bae, Myung Ae,Lee, Hohjai,Rhee, Sang Dal,Ahn, Jin Hee
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p. 3909 - 3914
(2017/07/27)
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- Mo(CO)6 as a Solid CO Source in the Synthesis of Aryl/Heteroaryl Weinreb Amides under Microwave-Enhanced Condition
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The facile transformation of aryl/heteroaryl nonaflates into corresponding amides via Pd-catalyzed aminocarbonylation using Mo(CO)6 as a solid CO source under microwave-enhanced condition is reported. The method was found to be tolerant with respect to a
- Ningegowda, Raghu,Bhaskaran, Savitha,Sajith, Ayyiliath M.,Aswathanarayanappa, Chandrashekar,Padusha, M. Syed Ali,Priya, Babu Shubha
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- Palladium-Catalyzed, ortho-Selective C-H Halogenation of Benzyl Nitriles, Aryl Weinreb Amides, and Anilides
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A palladium-catalyzed, ortho-selective C-H halogenation methodology is reported herein. The highlight of the work is the highly selective C(sp2)-H functionalization of benzyl nitriles in the presence of activated C(sp3)-H bond, which results in good yields of the halogenated products with excellent regioselectivity. Along with benzyl nitriles, aryl Weinreb amides and anilides have been evaluated for the transformation using aprotic conditions. Mechanistic studies yield interesting aspects with respect to the pathway of the reaction and the directing group abilities.
- Das, Riki,Kapur, Manmohan
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p. 1114 - 1126
(2018/06/18)
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- Synthesis of Difluoromethyl Ketones from Weinreb Amides, and Tandem Addition/Cyclization of o-Alkynylaryl Weinreb Amides
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[Difluoro(phenylsulfanyl)methyl]trimethylsilane (PhSCF2SiMe3) underwent a fluoride-induced nucleophilic addition to the carbonyl group of Weinreb amides to provide the corresponding difluoro(phenylsulfanyl)methyl ketones. These were
- Phetcharawetch, Jongkonporn,Betterley, Nolan M.,Soorukram, Darunee,Pohmakotr, Manat,Reutrakul, Vichai,Kuhakarn, Chutima
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supporting information
p. 6840 - 6850
(2017/12/26)
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- Design and synthesis of an activity-based protein profiling probe derived from cinnamic hydroxamic acid
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In our continued effort to discover new anti-hepatitis C virus (HCV) agents, we validated the anti-replicon activity of compound 1, a potent and selective anti-HCV hydroxamic acid recently reported by us. Generally favorable physicochemical and in vitro absorption, distribution, metabolism, and excretion (ADME) properties exhibited by 1 made it an ideal parent compound from which activity-based protein profiling (ABPP) probe 3 was designed and synthesized. Evaluation of probe 3 revealed that it possessed necessary anti-HCV activity and selectivity. Therefore, we have successfully obtained compound 3 as a suitable ABPP probe to identify potential molecular targets of compound 1. Probe 3 and its improved analogs are expected to join a growing list of ABPP probes that have made important contributions to not only the studies of biochemical and cellular functions but also discovery of selective inhibitors of protein targets.
- Ai, Teng,Qiu, Li,Xie, Jiashu,Geraghty, Robert J.,Chen, Liqiang
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p. 686 - 692
(2016/05/24)
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- ANTIDIABETIC BICYCLIC COMPOUNDS
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Novel compounds of the structural formula (I), and the pharmaceutically acceptable salts thereof, are agonists of G-protein coupled receptor 40 (GPR40) and may be useful in the treatment, prevention and suppression of diseases mediated by the G-protein-coupled receptor 40. The compounds of the present invention may be useful in the treatment of Type 2 diabetes mellitus, and of conditions that are often associated with this disease, including obesity and lipid disorders, such as mixed or diabetic dyslipidemia, hyperlipidemia, hypercholesterolemia, and hypertriglyceridemia.
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Page/Page column 90
(2016/04/26)
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- Discovery of 1,1′-Biphenyl-4-sulfonamides as a New Class of Potent and Selective Carbonic Anhydrase XIV Inhibitors
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New 1,1′-biphenylsulfonamides were synthesized and evaluated as inhibitors of the ubiquitous human carbonic anhydrase isoforms I, II, IX, XII, and XIV using acetazolamide (AAZ) as reference compound. The sulfonamides 1-21 inhibited all the isoforms, with Ki values in the nanomolar range of concentration, and were superior to AAZ against all of them. X-ray crystallography and molecular modeling studies on the adducts that compound 20, the most potent hCA XIV inhibitor of the series (Ki = 0.26 nM), formed with the five hCAs, provided insight into the molecular determinants responsible for the high affinity of this molecule toward the target enzymes. The results pave the way to the development of 1.1′-biphenylsulfonamides as a new class of highy potent hCA XIV inhibitors.
- La Regina, Giuseppe,Coluccia, Antonio,Famiglini, Valeria,Pelliccia, Sveva,Monti, Ludovica,Vullo, Daniela,Nuti, Elisa,Alterio, Vincenzo,De Simone, Giuseppina,Monti, Simona Maria,Pan, Peiwen,Parkkila, Seppo,Supuran, Claudiu T.,Rossello, Armando,Silvestri, Romano
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supporting information
p. 8564 - 8572
(2015/11/24)
-
- Synthesis and biological evaluation of N-cyclopropylbenzamide-benzophenone hybrids as novel and selective p38 mitogen activated protein kinase (MAPK) inhibitors
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A series of hybrid molecules consisting of benzophenones and N-cyclopropyl-3-methylbenzamides were synthesized and biologically evaluated as novel p38 mitogen activated protein kinase (MAPK) inhibitors. In particular, we found that compound 10g displayed
- Heo, Jinyuk,Shin, Hanbo,Lee, Jun,Kim, Taelim,Inn, Kyung-Soo,Kim, Nam-Jung
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p. 3694 - 3698
(2015/08/11)
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- Chiral silver phosphate catalyzed transformation of ortho-alkynylaryl ketones into 1H-isochromene derivatives through an intramolecular-cyclization/ enantioselective-reduction sequence
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The transformation of ortho-alkynylaryl ketones through a cyclization/enantioselective-reduction sequence in the presence of a chiral silver phosphate catalyst afforded 1H-isochromene derivatives in high yield with fairly good to high enantioselectivity. An asymmetric synthesis of the 9-oxabicyclo[3.3.1]nona-2,6-diene framework, which has been found in some biologically active molecules, is presented as a demonstration of the synthetic utility of this method. Dependent on its other half: The title reaction of ortho-alkynylaryl ketones in the presence of a silver catalyst with a chiral counteranion afforded 1H-isochromene derivatives in high yield with good to high enantioselectivity (see scheme; R1=alkyl, aryl; R2=aryl; R3=H, F). An asymmetric synthesis of the 9-oxabicyclo[3.3.1]nona-2,6- diene framework found in biologically active molecules highlights the synthetic utility of this method. Copyright
- Terada, Masahiro,Li, Feng,Toda, Yasunori
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supporting information
p. 235 - 239
(2014/01/17)
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- An Efficient synthesis of Weinreb amides and ketones via palladium nanoparticles on ZIF-8 catalysed carbonylative coupling
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Heterogeneously catalysed carbonylative coupling reactions such as aminocarbonylation and Suzuki-carbonylation are reported using Pd nanoparticles supported on ZIF-8 for efficient and environmentally attractive synthesis of Weinreb amides and ketones from aryl bromides or iodides. The catalyst is air stable, offers high activity with very low palladium leaching and is recyclable. The presence of a phosphine ligand was required when aryl bromides were used as substrates, while no ligand was necessary when aryl iodides were used. the Partner Organisations 2014.
- Thanh Dang, Tuan,Chen, Anqi,Majeed Seayad, Abdul
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p. 30019 - 30027
(2014/08/05)
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- Discovery of novel indazole derivatives as dual angiotensin II antagonists and partial PPARγ agonists
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Identification of indazole derivatives acting as dual angiotensin II type 1 (AT1) receptor antagonists and partial peroxisome proliferator-activated receptor-γ (PPARγ) agonists is described. Starting from Telmisartan, we previously described that indole derivatives were very potent partial PPARγ agonists with loss of AT1 receptor antagonist activity. Design, synthesis and evaluation of new central scaffolds led us to the discovery of pyrrazolopyridine then indazole derivatives provided novel series possessing the desired dual activity. Among the new compounds, 38 was identified as a potent AT1 receptor antagonist (IC50 = 0.006 μM) and partial PPARγ agonist (EC50 = 0.25 μM, 40% max) with good oral bioavailability in rat. The dual pharmacology of compound 38 was demonstrated in two preclinical models of hypertension (SHR) and insulin resistance (Zucker fa/fa rat).
- Lamotte, Yann,Faucher, Nicolas,Sancon, Julien,Pineau, Olivier,Sautet, Stephane,Fouchet, Marie-Helene,Beneton, Veronique,Tousaint, Jean-Jacques,Saintillan, Yannick,Ancellin, Nicolas,Nicodeme, Edwige,Grillot, Didier,Martres, Paul
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p. 1098 - 1103
(2014/03/21)
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- Synthesis of functionalised 4H-quinolizin-4-ones via tandem Horner-Wadsworth-Emmons olefination/cyclisation
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4H-Quinolizin-4-ones are a unique class of heterocycle with valuable physicochemical properties and which are emerging as key pharmacophores for a range of biological targets. A tandem Horner-Wadsworth-Emmons olefination/cyclisation method has been developed to allow facile access to substituted 4H-quinolizin-4-ones encoded with a range of functional groups.
- Muir, Calum W.,Kennedy, Alan R.,Redmond, Joanna M.,Watson, Allan J. B.
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supporting information
p. 3337 - 3340
(2013/06/05)
-
- Synthesis and in vitro biological evaluation of pyrazole group-containing analogues for PDE10A
-
Twenty eight new analogues were synthesized by optimizing the structure of MP-10 and their in vitro binding affinities towards PDE10A, PDE3A/B, and PDE4A/B were determined. Among these new analogues, 10a, 10b, 10d, 11a, 11b and 11d are very potent towards PDE10A and have IC50 values of 0.40 ± 0.02, 0.28 ± 0.06, 1.82 ± 0.25, 0.24 ± 0.05, 0.36 ± 0.03 and 1.78 ± 0.03 nM respectively; these six compounds displayed high selectivity for PDE10A versus PDE3A/3B/4A/4B. The promising compounds will be further validated in vivo to identify PDE10A imaging tracers. The Royal Society of Chemistry.
- Li, Junfeng,Jin, Hongjun,Zhou, Haiying,Rothfuss, Justin,Tu, Zhude
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p. 443 - 449
(2013/06/04)
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- ALKYNE-BRIDGED HETERO-AROMATICS AND USES THEREOF
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This invention relates to novel alkyne-bridged hetero-aromatics as described in the specification which are PDE10A inhibitors and useful for the treatment of neurological, psychiatric disorder, metabolic disorders, such as Schizophrenia, Parkinson's disea
- -
-
Paragraph 0303; 0304
(2013/06/28)
-
- Synthesis and structure-activity relationships of benzophenone-bearing diketopiperazine-type anti-microtubule agents
-
KPU-105 (4), a potent anti-microtubule agent that contains a benzophenone was derived from the diketopiperazine-type vascular disrupting agent (VDA) plinabulin 3, which displays colchicine-like tubulin depolymerization activity. To develop derivatives wit
- Hayashi, Yoshio,Yamazaki, Yuri,Sumikura, Makiko,Masuda, Yurika,Hayashi, Yoshiki,Yasui, Hiroyuki,Kiso, Yoshiaki,Chinen, Takumi,Usui, Takeo,Yakushiji, Fumika,Potts, Barbara,Neuteboom, Saskia,Palladino, Michael,Lloyd, George Kenneth
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experimental part
p. 4279 - 4289
(2012/09/08)
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- Analogues of fenarimol are potent inhibitors of trypanosoma cruzi and are efficacious in a murine model of chagas disease
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We report the discovery of nontoxic fungicide fenarimol (1) as an inhibitor of Trypanosoma cruzi (T. cruzi), the causative agent of Chagas disease, and the results of structure-activity investigations leading to potent analogues with low nM IC50s in a T. cruzi whole cell in vitro assay. Lead compounds suppressed blood parasitemia to virtually undetectable levels after once daily oral dosing in mouse models of T. cruzi infection. Compounds are chemically tractable, allowing rapid optimization of target biological activity and drug characteristics. Chemical and biological studies undertaken in the development of the fenarimol series toward the goal of delivering a new drug candidate for Chagas disease are reported.
- Keenan, Martine,Abbott, Michael J.,Alexander, Paul W.,Armstrong, Tanya,Best, Wayne M.,Berven, Bradley,Botero, Adriana,Chaplin, Jason H.,Charman, Susan A.,Chatelain, Eric,Von Geldern, Thomas W.,Kerfoot, Maria,Khong, Andrea,Nguyen, Tien,McManus, Joshua D.,Morizzi, Julia,Ryan, Eileen,Scandale, Ivan,Thompson, R. Andrew,Wang, Sen Z.,White, Karen L.
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p. 4189 - 4204
(2012/07/27)
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- Ru-catalyzed hydrogenation of 3,5-diketo amides: Simultaneous control of chemo- and enantioselectivity
-
By modulating the chelating priorities of the different directing groups in 3,5-diketo amides with the assistance from coordinating solvent, highly chemo- and enantioselective hydrogenation of the C3-carbonyls was achieved in the presence of [RuCl(benzene)(S)-SunPhos]Cl in THF.
- Li, Wanfang,Fan, Weizheng,Ma, Xin,Tao, Xiaoming,Li, Xiaoming,Xie, Xiaomin,Zhang, Zhaoguo
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supporting information
p. 8976 - 8978
(2012/11/07)
-
- Synthesis and pharmacological evaluation of 3-aryl-3-azolylpropan-1-amines as selective triple serotonin/norepinephrine/dopamine reuptake inhibitors
-
A series of 3-aryl-3-azolylpropan-1-amines was prepared and screened for its capability of inhibiting monoamine reuptake. Analogs with nanomolar potency, good human in vitro microsomal stability, and low drug-drug interaction potential were described. In
- Lee, Ki-Ho,Park, Chun-Eung,Min, Kyung-Hyun,Shin, Yong-Je,Chung, Coo-Min,Kim, Hui-Ho,Yoon, Hae-Jeoung,Won-Kim,Ryu, Eun-Ju,Shin, Yu-Jin,Nam, Hyun-Sik,Cho, Jeong-Woo,Lee, Hee-Yoon
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scheme or table
p. 5567 - 5571
(2010/12/29)
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- Discovery of biphenylketones as dual modulators of inflammation and bone loss
-
Biphenylketones were identified as novel inhibitors of NFκB activation. Structure-activity studies led to the identification of compound 4c, which had good potency against osteoclasts (IC50 = 0.8 μM), showed oral activity, and was able to compl
- Greig, Iain R.,Coste, Emmanuel,Ralston, Stuart H.,Van'T Hof, Rob J.
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supporting information; experimental part
p. 5548 - 5551
(2010/12/29)
-
- Design, synthesis, and biological evaluation of potent thiosemicarbazone based cathepsin L inhibitors
-
A small library of 36 functionalized benzophenone thiosemicarbazone analogs has been prepared by chemical synthesis and evaluated for their ability to inhibit the cysteine proteases cathepsin L and cathepsin B. Inhibitors of cathepsins L and B have the potential to limit or arrest cancer metastasis. The six most active inhibitors of cathepsin L (IC50 50 > 10,000 nM). The most active analog in the series, 3-bromophenyl-2′-fluorophenyl thiosemicarbazone 1, also efficiently inhibits cell invasion of the DU-145 human prostate cancer cell line.
- Kishore Kumar,Chavarria, Gustavo E.,Charlton-Sevcik, Amanda K.,Arispe, Wara M.,MacDonough, Matthew T.,Strecker, Tracy E.,Chen, Shen-En,Siim, Bronwyn G.,Chaplin, David J.,Trawick, Mary Lynn,Pinney, Kevin G.
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supporting information; experimental part
p. 1415 - 1419
(2010/07/06)
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- TRIAZOLOPYRIDINE JAK INHIBITOR COMPOUNDS AND METHODS
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A compound of Formula I, enantiomers, diasteriomers, tautomers or pharmaceutically acceptable salts thereof, wherein R1, R2, R3, R4 and R5 are defined herein, are useful as JAK kinase inhibitors. A ph
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Page/Page column 98-99
(2010/01/12)
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- 5-Aryl-indan-1-ol and analogs useful as progesterone receptor modulators
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Compounds of formula I are provided, wherein R1-R9 and n are defined herein, and pharmaceutical compositions and kits containing these compounds. Also provided are methods of inducing contraception, providing hormone replacement ther
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-
Page/Page column 15
(2010/11/26)
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- 5-Aryl-indan-1-one and analogs useful as progesterone receptor modulators
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Compounds of formula I or II are provided, wherein R1—R8 are defined herein, and pharmaceutical compositions and kits containing these compounds. Also provides are methods of inducing contraception, providing hormone replacement ther
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Page/Page column 16
(2010/11/26)
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- CHEMICAL COMPOUNDS
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The present invention relates to novel compounds with a variety of therapeutic uses, more particularly novel substituted cyclic alkylidene compounds that are particularly useful for selective estrogen receptor modulation.
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Page/Page column 80
(2008/06/13)
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- The sydnone ring as an ortho-director of lithiation. 2. Dilithiation of 3-phenylsydnone and regiospecific @?o-aryl acylation using N-methoxy-N-methylamides
-
Readily available 3-phenylsydnone (1) reacts with n-butyllithium/TMEDA to form the dilithio species 2 which can be regiospecifically acylated at the ortho-aryl position using N-methoxy-N-methylamides (Weinreb's amides).
- Turnbull, Kenneth,Sun, Congcong,Krein, Douglas M.
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p. 1509 - 1512
(2007/10/03)
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