- Preparation method of O-diphenyl phosphoryl hydroxylamine
-
The invention provides a preparation method of O-diphenyl phosphoryl hydroxylamine, wherein the preparation method is characterized by comprising the following steps: S1, reacting benzyl N-hydroxycarbamate with diphenyl phosphinyl chloride in a first solvent under the action of organic alkali to generate an intermediate, namely N-benzyloxycarbonyl-O-diphenyl phosphoryl hydroxylamine; and S2, carrying out reduction hydrogenation reaction on the intermediate in a second solvent under the action of a metal catalyst to remove a N-benzyloxycarbonyl protecting group, and thus obtaining the O-diphenyl phosphoryl hydroxylamine. According to the preparation method of the O-diphenyl phosphoryl hydroxylamine compound disclosed by the embodiment of the invention, Cbz-hydroxylamine with a protecting group is used as a raw material to react with diphenyl phosphinyl chloride, so that the selectivity of O-phosphonyl protection is improved, and the production cost is reduced; the whole operation is carried out under an alkaline condition, the stability of oxygen-phosphorus bonds can be maintained, and the generation of diphenyl hypophosphorous acid byproducts is avoided, so that the intermediate can be directly used for the next step of reaction.
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Paragraph 0053; 0060-0064; 0065; 0070-0072
(2021/03/30)
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- PDE9 INHIBITORS FOR TREATMENT OF PERIPHERAL DISEASES
-
The present invention relates to PDE9 inhibitors, their synthesis, and their use for treatment of benign prostate hyperplasia, beta thalassemia, and sickle cell disease.
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Paragraph 00195; 00286-00288
(2018/09/25)
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- PDE9 INHIBITORS WITH IMIDAZO TRIAZINONE BACKBONE AND IMIDAZO PYRAZINONE BACKBONE FOR TREATMENT OF PERIPHERAL DISEASES
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The present invention relates to PDE9 inhibitors and their use for treatment of benign prostate hyperplasia and sickle cell disease.
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Page/Page column 57
(2017/02/09)
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- COMPOSITIONS USEFUL FOR TREATING DISORDERS RELATED TO KIT
-
Compounds and compositions useful for treating disorders related to Kit are described herein.
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Paragraph 0083-0084
(2016/04/26)
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- COMPOSITIONS USEFUL FOR TREATING DISORDERS RELATED TO KIT
-
Compounds and compositions useful for treating disorders related to mutant KIT are described herein.
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Paragraph 0177; 0178
(2015/04/28)
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- HETEROCYCLIC MODULATORS OF LIPID SYNTHESIS AND COMBINATIONS THEREOF
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Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by disregulation of a fatty acid synthase pathway by the administration of such compounds and combinations of such compounds and other therapeutic agents.
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Page/Page column 149; 150
(2015/07/07)
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- HETEROCYCLIC MODULATORS OF LIPID SYNTHESIS
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Heterocyclic modulators of lipid synthesis are provided as well as pharmaceutically acceptable salts thereof; pharmaceutical compositions comprising such compounds; and methods of treating conditions characterized by disregulation of a fatty acid synthase pathway by the administration of such compounds.
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Page/Page column 134; 135
(2014/01/18)
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- POTASSIUM CHANNEL MODULATORS
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Disclosed herein are KCNQ potassium channels modulators of formula (I) wherein ring Z1, R1, p, R3, and R4 are as defined in the specification. Compositions comprising such compounds; and methods for treating conditions and disorders using such compounds and compositions are also described.
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Page/Page column 24
(2011/06/19)
-
- Amine-promoted synthesis of vinyl aziridines
-
N-Unsubstituted vinyl aziridines were synthesized via an amine-promoted regioselective nucleophilic aziridination of α,β,γ,δ- unsaturated carbonyl compounds. The reaction is completely regioselective (>95: 5) for the α,β-alkene and completely diastereosel
- Armstrong, Alan,Pullin, Robert D. C.,Jenner, Chloe R.,Scutt, James N.
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supporting information; experimental part
p. 3499 - 3502
(2010/08/06)
-
- Novel Inhibitors of Hepatitis C Virus Replication
-
The embodiments provide compounds of the general Formula I, as well as compositions, including pharmaceutical compositions, comprising a subject compound. The embodiments further provide treatment methods, including methods of treating a hepatitis C virus infection and methods of treating liver fibrosis, the methods generally involving administering to an individual in need thereof an effective amount of a subject compound or composition.
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Page/Page column 91-92
(2009/10/21)
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- Fischer synthesis of isomeric thienopyrrole LHRH antagonists
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As part of a structure-activity exploration into LHRH antagonists, structures containing the thieno[2,3-b]pyrrole core were identified as potent antagonists. This letter describes the employment of the Fischer synthesis to access this thienopyrrole and isomeric final compounds.
- Andrews, David M.,Arnould, Jean-Claude,Boutron, Pascal,Délouvrie, Bénédicte,Delvare, Christian,Foote, Kevin M.,Hamon, Annie,Harris, Craig S.,Lambert-van der Brempt, Christine,Lamorlette, Maryannick,Matusiak, Zbegniew M.
-
experimental part
p. 5805 - 5816
(2009/12/24)
-
- 1H-Indole-Pyridinecarboxamide and 1H-Indole-Piperidinecarboxamide Compounds
-
Compounds of formula (I): wherein: A represents a divalent radical: wherein: Z represents an oxygen atom or a sulphur atom,R6 represents a hydrogen atom, an alkyl, alkenyl, arylalkyl or polyhaloalkyl group or a substituted, linear or branched alkyl chain, represents a single bond or a double bond,R1, R2, R3 and R4 represent a hydrogen or halogen atom,an alkyl, alkoxy, hydroxy, cyano, nitro, polyhaloalkyl or optionally substituted amino group, or a linear or branched alkyl chain substituted by one or more groups,R5 represents a hydrogen atom or an alkyl, aminoalkyl or hydroxyalkyl group,X and Y represent a hydrogen atom or an alkyl group,Ra, Rb, Rc and Rd represent a hydrogen or halogen atom, an alkyl, hydroxy, alkoxy, cyano, nitro, polyhaloalkyl, optionally substituted amino group, or a substituted, linear or branched alkyl chain,Re represents a hydrogen atom or an alkyl, arylalkyl or alkenyl group or a substituted, linear or branched alkyl chain, their enantiomers, diastereoisomers, and N-oxides, and also addition salts thereof with a pharmaceutically acceptable acid or base.
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Page/Page column 6
(2009/10/21)
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- USE OF NEUROPROTECTIVE COMPOUNDS IN OBTAINING MEDICAMENTS INTENDED FOR THE TREATMENT OF NEURODEGENERATING DISEASES
-
Use of neuroprotective compounds in obtaining medicaments intended for the curative treatment of neurodegenerative disease and/or the prevention of the appearance of disorders ensuing from those diseases.
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- SUBSTITUTED 4-AMINO-PYRROLOTRIAZINE DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS AND DISEASES ASSOCIATED WITH ANGIOGENESIS
-
This invention relates to novel pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds and compositions for the prevention and/or treatment of hyper-proliferative disorders and diseases associated with angiogenesis.
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Page/Page column 190
(2008/06/13)
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- Amine-promoted, organocatalytic aziridination of enones
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(Chemical Equation Presented) A novel method is presented using N-N ylides (prepared by in situ amination of a tertiary amine) for the aziridination of a range of enone systems. The amine may be used sub-stoichiometrically, and promising levels of enantioselectivity are observed with quinine as promoter.
- Armstrong, Alan,Baxter, Carl A.,Lamont, Scott G.,Pape, Andrew R.,Wincewicz, Richard
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p. 351 - 353
(2007/10/03)
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- PYRROLOTRIAZINE DERIVATIVES USEFUL FOR TREATING CANCER THROUGH INHIBITION OF AURORA KINASE
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This invention relates to novel compounds and processes for their preparation, methods of treating diseases, particularly Cancer, comprising administering said compounds, and methods of making pharmaceutical compositions for the treatment or prevention of
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Page/Page column 46-47
(2010/11/27)
-
- Catalytic enantioselective indium-mediated allylation of hydrazones
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(Chemical Equation Presented) A facile and highly selective indium-mediated allylation of hydrazones utilizing BINOL ligands is described. Chiral (R)-3,3′-bistrifluoromethylBINOL afforded homoallylic amines in up to 97% ee with stoichiometric ligand. Employing only 10 mol % ligand afforded selectivity of up to 92% ee.
- Cook, Gregory R.,Kargbo, Robert,Maity, Bikash
-
p. 2767 - 2770
(2007/10/03)
-
- PYRROLOTRIAZINE DERIVATIVES USEFUL FOR TREATING HYPER-PROLIFERATIVE DISORDERS AND DISEASES ASSOCIATED WITH ANGIOGENESIS
-
This invention relates to pyrrozolotriazine compounds, pharmaceutical compositions containing such compounds and the use of those compounds and compositions for the prevention and/or treatment of hyper-proliferative disorders and diseases associated with angiogenesis.
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Page/Page column 68; 69
(2008/06/13)
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- PYRROLOPYRIDAZINE DERIVATIVES
-
The invention relates to compound of the formula (I) or its salt, in which R1, R2, R3 and R4 are as defined in the description, their use of as medicament, the process for their preparation and use for the treatment of PDE-IV or TNF-α mediated diseases.
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-
- Asymmetric Total Synthesis of an Important 3-(Hydroxymethyl)carbacephalosporin
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Carbacephalosporins have gained much attention as important antibacterial agents. Recently, 3-(hydroxymethyl)carbacephalosporins have been linked to quinolones for the production of multifunctional antibiotics. A short, practical asymmetric total synthesis of carbacephalosporin 3, suitable for conjugating to other chemical moieties, is reported. The synthesis was achieved by Mitsunobu cyclization of dipeptide 12, prepared from L-erythro-anti-β-hydroxy-α-amino acid 11, and subsequent Horner-Wadsworth-Emmons cyclization of ketone 16.
- Stocksdale, Mark G.,Ramurthy, Savithri,Miller, Marvin J.
-
p. 1221 - 1225
(2007/10/03)
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- Aminations with O-Diphenylphosphinylhydroxylamine. A Critical Evaluation
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A critical evaluation is presented of the scope of amination reactions with O-diphenylphosphinylhydroxylamine (ODPH) as compared to those using hydroxylamine-O-sulfonic acid (HOSA).Aminations with ODPH of isopropyl, t-butyl and cyclohexyl carbanions derived from the corresponding Grignard reagents, gave the corresponding amines in 36, 34 and 50 percent yields, respectively.The amination with HOSA of the same carbanions under similar conditions was unsuccessful.The aminative quaternization of the tertiary nitrogen of pyridine and quinoline with ODPH proceeded with comparable yields to those obtained with HOSA.An improved one flask amination with ODPH of indole, skatole and carbazole was achieved in 52 - 62 percent yields.The amination under the same conditions using HOSA gave consistently lower yields.Several other amination reactions which have been reported for HOSA were unsuccessful using ODPH.The conclusion is reached that overall the ODPH reagent is much less versatile than HOSA.Nevertheless, in the aminations of NH groups of heterocyclic compounds ODPH appears to be superior to HOSA and is the reagent of choice, in particular, since the preparation of ODPH is much less harzardous than that of HOSA. - Keywords: Synthesis, O-Diphenylphosphinylhydroxylamine, Hydroxylamine-O-sulfonic Acid, N-Amino Derivatives, N-Amino Heterocyclic Compounds
- Sosnovsky, George,Purgstaller, Klaus
-
p. 582 - 586
(2007/10/02)
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- METHOXY-CATALYSED REARRANGEMENT OF N- TO O-(DIPHENYLPHOSPHINYL)HYDROXYLAMINE
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In methanol Ph2P(O)NHOH undergoes rapid NaOMe-catalysed rearrangement to Ph2P(O)ONH2 which is subsequently converted into Ph2P(O)ONa and Ph2P(O)OMe.
- Harger, Martin J. P.
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p. 3115 - 3116
(2007/10/02)
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- O-(DIPHENYLPHOSPHINYL)HYDROXYLAMINE: A NEW REAGENT FOR ELECTROPHILIC C-AMINATION
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O-(Diphenylphosphinyl)hydroxylamine efficiently aminates a variety of stabilised carbanions and certain Grignard reagents.
- Colvin, Ernest W.,Kirby, Gordon W.,Wilson, Arthur C.
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p. 3835 - 3836
(2007/10/02)
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- O-(Diphenylphosphinyl)hydroxylamine: Preparation and Some Characteristic Chemical Reactions
-
Hydroxylamine reacts with diphenylphosphinic chloride (1) in benzene (or aqueous dioxan) to give O-(diphenylphosphinyl)hydroxylamine (3) and not the N-phosphinyl compound (2) as was previously thought.Di-p-tolyl-, bis-p-methoxyphenyl-, and phenyl-p-methox
- Harger, Martin J. P.
-
p. 3284 - 3288
(2007/10/02)
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