- 3-(Methoxycarbonyl)Cyclobutenone as a Reactive Dienophile in Enantioselective Diels–Alder Reactions Catalyzed by Chiral Oxazaborolidinium Ions
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Cyclobutenone has been used as a highly reactive dienophile in Diels–Alder reactions, however, no enantioselective example has been reported. We disclose herein a chiral oxazaborolidine-aluminum bromide catalyzed enantioselective Diels–Alder reaction of 3-alkoxycarbonyl cyclobutenone with a variety of dienes. Furthermore, a total synthesis of (?)-kingianin F was completed for the first time via enantioenriched cycloadduct bicyclo[4.2.0]octane derivative.
- Yan, Peng,Zhong, Changxu,Zhang, Jie,Liu, Yu,Fang, Huayi,Lu, Ping
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- Palladium-Catalyzed Carbene Coupling Reactions of Cyclobutanone N-Sulfonylhydrazones
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Described herein are the palladium-catalyzed cross-coupling reactions of cyclobutanone-derived N-sulfonylhydrazones with aryl or benzyl halides, suggesting that the metal carbene process and β-hydride elimination can smoothly occur in strained ring system
- Ning, Xiaoqin,Chen, Yongke,Hu, Fangdong,Xia, Ying
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supporting information
p. 8348 - 8352
(2021/10/25)
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- INTERMEDIATE COMPOUNDS AND METHDODS
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The present invention relates to compounds of (II) and an acceptable salt or hydrate thereof method of making same.
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Page/Page column 7
(2019/02/15)
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- PROCESS FOR THE PREPARATION OF AN AMINO-PYRIMIDINE AND INTERMEDIATES THEREOF
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Provided herein is a novel process for the preparation of an amino-pyrimidine and salts thereof. Also provided herein are novel intermediates used in this process and their preparation.
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Paragraph 0096
(2019/07/17)
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- FUSED PENTACYCLIC IMIDAZOLE DERIVATIVES AS MODULATORS OF TNF ACTIVITY
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A compound of formula (I) as defined herein, or a pharmaceutically acceptable salt thereof, being potent modulators of human TNFα activity, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
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Page/Page column 40
(2018/11/22)
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- Method for synthesizing 3-(Boc-aminomethyl)cyclobutanone
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The invention relates to a method for synthesizing 3-(Boc-aminomethyl)cyclobutanone. The method for synthesizing 3-(Boc-aminomethyl)cyclobutanone provided by the invention mainly solves the technicalproblems of high raw material cost and relatively diffic
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Paragraph 0005; 0007
(2019/01/08)
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- FUSED PENTACYCLIC IMIDAZOLE DERIVATIVES AS MODULATORS OF TNF ACTIVITY
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A series of substituted fused pentacyclic imidazopyridine and imidazopyridazine derivatives, and analogues thereof, being potent modulators of human TNFα activiy, are accordingly of benefit in the treatment and/or prevention of various human ailments, including autoimmune and inflammatory disorders; neurological and neurodegenerative disorders; pain and nociceptive disorders; cardiovascular disorders; metabolic disorders; ocular disorders; and oncological disorders.
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Page/Page column 96
(2018/10/19)
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- COMPOUNDS THAT INHIBIT MCL-1 PROTEIN
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Provided herein are myeloid cell leukemia 1 protein (Mcl-1) inhibitors, methods of their preparation, related pharmaceutical compositions, and methods of using the same. For example, provided herein are compounds of Formula I, and pharmaceutically acceptable salts thereof and pharmaceutical compositions containing the compounds. The compounds and compositions provided herein may be used, for example, in the treatment of diseases or conditions, such as cancer.
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Page/Page column 337
(2017/09/15)
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- Containing cyclobutane substituent of pyrazines, its composition and use thereof
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The invention relates to a cyclobutane substituent group-containing pyrazine compound and application thereof as a drug, and particularly relates to application of the cyclobutane substituent group-containing pyrazine compound in preparing the drug for preventing and treating various influenza viruses. Especially, the invention relates to a compound as shown in a general formula (I) or a stereomer, a geometrical isomer, a tautomer, a nitrogen oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and various variables are defined in the specification. The invention also relates to application of the compound as shown in the general formula (I) or the stereomer, geometrical isomer, tautomer, nitrogen oxide, hydrate, solvate, metabolite, pharmaceutically acceptable salt or prodrug thereof as the drug, and particularly relates to application of the compound as shown in the general formula (I) or the stereomer, geometrical isomer, tautomer, nitrogen oxide, hydrate, solvate, metabolite, pharmaceutically acceptable salt or prodrug thereof as the drug for preventing and treating the influenza viruses.
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- Containing cyclobutane substituent of pyrazines, its composition and use thereof
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The invention relates to a pyrazine compound containing a diethylene substituent and application thereof as a medicine, particularly application thereof to preparation of medicines for preventing and treating various influenza viruses. Particularly, the invention relates a compound of which the general formula I is shown in the specification, or a stereoisomer, a geometrical isomer, a tautomer, a nitrogen oxide, a hydrate, a solvate, a metabolite, a pharmaceutically acceptable salt or a prodrug thereof, and all variables are defined in the specification. The invention also relates to application of the compound of which the general formula I is shown in the specification, or the stereoisomer, the geometrical isomer, the tautomer, the nitrogen oxide, the hydrate, the solvate, the metabolite, the pharmaceutically acceptable salt or the prodrug thereof as medicines, particularly application of the compound as a medicine for preventing and treating influenza viruses.
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- Substituted purine neuraminidase inhibitor and method of use thereof, and use thereof
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The invention provides novel substituted purine compounds or stereoisomers, tautomers, nitric oxides, solvates, metabolites and pharmaceutically acceptable salts or prodrugs thereof. The substituted purine compounds are used for inhibiting neuraminidase. The invention also provides a drug composition comprising the compounds, and a method for preventing or treating virus infectious diseases by using the compounds or the drug composition.
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- OXAZOLIDINONES AS MODULATORS OF MGLUR5
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The disclosure generally relates to compounds of formula I, including their salts, as well as compositions and methods of using the compounds. The compounds are ligands, agonists and partial agonists for the mGluR5 receptor and may be useful for the treatment of various disorders of the central nervous system.
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Page/Page column 35
(2015/04/28)
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- INHIBITORS OF ARGINASE AND THEIR THERAPEUTIC APPLICATIONS
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The inventive compounds are small molecule therapeutics that are potent inhibitors of Arginase I and II activity. The invention also provides pharmaceutical compositions of the inventive compounds and methods for using the inventive compounds for treating or preventing a disease or a condition associated with arginase activity.
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Paragraph 0142-0143
(2013/05/09)
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- HETEROARYL AMIDES AS TYPE I GLYCINE TRANSPORT INHIBITORS
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The present invention relates to a series of substituted heteroaryl amides of the Formula I, wherein HET, A, X1 -X4, and R1-R12 groups are defined as in the specification, that exhibit activity as glycine transport inhibitors, their pharmaceutically acceptable salts, pharmaceutical compositions containing them, and their use for the enhancement of cognition and the treatment of the positive and negative symptoms of schizophrenia and other psychoses in mammals, including humans.
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Page/Page column 32; 33
(2008/12/06)
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- OXINDOLE DERIVATIVE AS FEEDING CONTROL AGENT
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Disclosed is a compound represented by the formula (1) below, a prodrug thereof or a pharmaceutically acceptable salt of either, which is useful as a therapeutic, preventive or ameliorating agent for diabetes and the like. (In the formula, R3 represents an optionally substituted carbamoyl group or the like; X represents a hydroxyl group or the like; W1 and W2 independently represent a single bond or methylene; R7 and R8 independently represent a hydrogen atom, an optionally substituted alkyl group or the like; and Ar represents an optionally substituted aryl group or the like.)
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Page/Page column 22
(2008/12/06)
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- 1-(1-CYCLOBUTYL-4-PIPERIDINYL)-1,3-DIHYDRO-2H-BENZIMIDAZOL-2-ONE DERIVATIVES WHICH HAVE ACTIVITY ON THE ML RECEPTOR AND THEIR USE IN MEDICINE
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Compounds of formula I or a salt thereof are provided wherein R4, R5, R6, Q, L and R are as defined in the description. Uses of the compounds as medicaments and in the manufacture of medicaments for treating psychotic disorders and cognitive impairments are disclosed. The invention further discloses pharmaceutical compositions comprising the compounds.
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Page/Page column 46
(2008/12/04)
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- Pyrazole glucokinase activators
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Disclosed herein are pyrazole glucokinase activators of the formula (I) useful for the treatment of metabolic diseases and disorders, preferably diabetes mellitus.
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Page/Page column 83
(2008/06/13)
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- AMINO CYCLOBUTYLAMIDE MODULATORS OF CHEMOKINE RECEPTOR ACTIVITY
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The present invention is directed to compounds of the formulas I and II : wherein R1, R2, R3, R4, R5, R6, R7, R8, R9, R10, R15, R16, R17, R18, R19, R25, R26, Y, Z, l, m, n and the broken lines are as defined herein which are useful as modulators of chemokine receptor activity. In particular, these compounds are useful as modulators of the chemokine receptor CCR-2.
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- A new entry into 2-azabicyclo[2.1.1]hexanes via 3-(chloromethyl)cyclobutanone
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2-Azabicyclo[2.1.1]hexanes, which possess the skeleton of 2,4-methanoproline (a naturally occurring insect antifeedant), were synthesized by imination of the previously unknown 3-(chloromethyl)cyclobutanone and subsequent reductive cyclization. The precursor of the latter, 3-oxocyclobutane carboxylic acid, was prepared by two pathways in multigram quantities.
- Stevens,De Kimpe
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p. 2174 - 2178
(2007/10/03)
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- FORMATION AND STABILITY OF ALKOXYIMIDATES IN THE CYCLOBUTANE BICYCLOBUTANE SYSTEM
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The reactions of CN- with methyl-3-chlorobicyclobutanecarboxylate and 3-chloro and 3-bromobicyclobutanecarbonitrile in MeOH were investigated.The MeO- present in the reaction mixture adds reversibly to the carbonitrile function of the various products.The equilibrium constants for the imidate formation were determined.The general notion that the imidate form is favored by an electron withdrawing group was reconfirmed.The order found was CN>ClBr>C(NH)OMe>CO2Me.It was also found that the central bond of bicyclobutane is a good mediator for transmittance of electronic effects.The unique stability of the alkoxyimidates compared to the low stability of the corresponding adducts with CN- is discussed.
- Hoz, S.,Aurbach, D.
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p. 1307 - 1314
(2007/10/02)
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