- Biquaternary ammonium compound and preparation method and application thereof
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The invention provides a biquaternary ammonium compound and a preparation method and application thereof. The biquaternary ammonium compound is shown as a formula (I). The compound disclosed by the invention has quick-acting and ultra-short-acting non-depolarized muscle relaxation molecular activity, is quick in acting and can generate a complete muscle relaxation effect under the condition of low administration dosage, and the time required for complete recovery of muscle strength is short and is obviously shorter than that of a positive drug cisatracurium and a depolarized muscle relaxation drug succinylcholine; the problems of non-depolarized muscle relaxant in the prior art are effectively solved, and the compound can be used for preparing the non-depolarized muscle relaxant with an excellent effect and has a good prospect.
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Paragraph 0142-0145
(2021/06/02)
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- A Universal Labeling Strategy for Nucleic Acids in Expansion Microscopy
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Expansion microscopy (ExM) enables the nanoscale imaging of ribonucleic acids (RNAs) on a conventional fluorescence microscope, providing information on the intricate patterns of gene expression at (sub)cellular resolution and within spatial context. To extend the use of such strategies, we examined a series of multivalent reagents that allow the labeling and grafting of deoxyribonucleic acid (DNA) oligonucleotide probes in a unified approach. We show that the reagents are directly compatible with third-generation in situ hybridization chain reaction RNA FISH (fluorescence in situ hybridization) techniques while displaying complete retention of the targeted transcripts. Furthermore, we validate and demonstrate that our labeling method is compatible with multicolor staining. Through oligonucleotide-conjugated antibodies, we demonstrate excellent performance in ×4 ExM and ×10 ExM, achieving a resolution of ～50 nm in ×10 ExM for both pre- and postexpansion labeling strategies. Our results indicate that our multivalent molecules enable the rapid functionalization of DNA oligonucleotides for ExM.
- Hofkens, Johan,Leen, Volker,Rohand, Taoufik,Vandereyken, Katy,Vanheusden, Marisa,Voet, Thierry,Wen, Gang
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supporting information
p. 13782 - 13789
(2021/09/11)
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- CRYSTAL FORM OF MONOMETHANESULFONATE OF DEUTERATED 3-(4,5-SUBSTITUTED AMINOPYRIMIDINE)PHENYL COMPOUND AND PREPARATION METHOD THEREFOR
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Disclosed in the present invention are a crystal form of monomethanesulfonate of a deuterated 3-(4,5-substituted aminopyrimidine)phenyl compound as represented by formula I, and a preparation method therefor. The crystal form is highly stable, can be used for treatment or prevention of diseases or conditions by means of epidermal growth factor receptors (EGFRs) in some mutation forms, can effectively inhibit the growth of a variety of tumor cells, and have an inhibiting effect on other proteases of EGFR and Her families, and thus can be used for preparing antitumor drugs.
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Paragraph 0047
(2021/02/26)
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- Ru-Catalyzed Switchable N-Hydroxyethylation and N-Acetonylation with Crude Glycerol
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Highly efficient Ru-catalyzed selective C?C or C?O bond cleavage of polyols (e.g., crude glycerol) for N-hydroxyethylation or N-acetonylation of amines was achieved through the hydrogen-borrowing approach. A variety of amines were transformed to the desired amino alcohols/ketones in moderate-to-excellent yields, opening up new avenues for generation of oxygenated pharmaceuticals and fine chemicals from renewable raw materials. The use of new redox-active catalysts containing bisphosphine/thienylmethylamine ligands allows this hydrogen-borrowing system to be operated selectively under both basic and acidic conditions.
- Xin, Zhuo,Jia, Le,Huang, Yuxing,Du, Chen-Xia,Li, Yuehui
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p. 2007 - 2011
(2020/03/19)
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- DEUTERATED 3-(4,5-SUBSTITUTED PYRIMIDINAMINE) PHENYL DERIVATIVES AND APPLICATIONS THEREOF
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The present invention discloses a type of deuterated 3-(4,5-substituted aminopyrimidine)phenyl derivatives and use thereof. The derivatives are compounds of Formula (I) or pharmaceutically acceptable salts thereof. These compounds or salts thereof can be used for treatment or prevention of diseases or illnesses through certain mutant forms of epidermal growth factor receptors, inhibit the growth of various tumor cells effectively, and inhibit other proteases of EGFR and Her families, they can be used for preparing anti-tumor drugs.
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Paragraph 0025-0028; 0079-0082
(2019/06/27)
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- METHOD OF PRODUCING TERTIARY AMINE OR TERTIARY AMINE DERIVATIVE
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PROBLEM TO BE SOLVED: To provide a method of producing tertiary amine or tertiary amine derivative with high selectivity. SOLUTION: In the method of producing tertiary amine or tertiary amine derivative, a reaction system including: an organic chemical raw material containing at least one kind of group selected from -NH2, -NH2 HCl, >NH and >NH HCl, a nitrogen atom contained in the group bounding to a carbon atom; aliphatic alcohol having 1 to 20 carbon atoms; and a catalyst where a carrier containing titanium oxide carries a silver component (metal silver or silver compound), is irradiated with light, and the group in the organic compound raw material is converted to -NR02 or >NR0, ( R0 is an aliphatic hydrocarbon group having 1 to 20 carbon atoms derived from the aliphatic alcohol). The percentage content of the silver in the catalyst is 0.5 to 10 mass% with respect to the titanium oxide. COPYRIGHT: (C)2015,JPOandINPIT
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Paragraph 0066; 0071
(2018/10/31)
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- Benzoxazolone Carboxamides as Potent Acid Ceramidase Inhibitors: Synthesis and Structure-Activity Relationship (SAR) Studies
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Ceramides are lipid-derived intracellular messengers involved in the control of senescence, inflammation, and apoptosis. The cysteine amidase, acid ceramidase (AC), hydrolyzes these substances into sphingosine and fatty acid and, by doing so, regulates their signaling activity. AC inhibitors may be useful in the treatment of pathological conditions, such as cancer, in which ceramide levels are abnormally reduced. Here, we present a systematic SAR investigation of the benzoxazolone carboxamides, a recently described class of AC inhibitors that display high potency and systemic activity in mice. We examined a diverse series of substitutions on both benzoxazolone ring and carboxamide side chain. Several modifications enhanced potency and stability, and one key compound with a balanced activity-stability profile (14) was found to inhibit AC activity in mouse lungs and cerebral cortex after systemic administration. The results expand our arsenal of AC inhibitors, thereby facilitating the use of these compounds as pharmacological tools and their potential development as drug leads.
- Bach, Anders,Pizzirani, Daniela,Realini, Natalia,Vozella, Valentina,Russo, Debora,Penna, Ilaria,Melzig, Laurin,Scarpelli, Rita,Piomelli, Daniele
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supporting information
p. 9258 - 9272
(2015/12/23)
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- Nucleophilic Fluorination and Radiofluorination via Aziridinium Intermediates: N-Substituent Influence, Unexpected Regioselectivity, and Differences between Fluorine-19 and Fluorine-18
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The efficient dehydrofluorination and radiofluorination of N,N-disubstituted-β-aminoalcohols through an anchimeric-assisted mechanism was developed. An investigation into the influence of N-substituents on the ring opening of the aziridinium intermediate indicated differences in the isomeric ratio and the yields of fluorinated products obtained from N,N-disubstituted-phenylalaninol. This influence was substantial for 18F-radiofluorination, with yields varying from 0 to 71% at room temperature (RT). Although no significant effects were observed in the fluorine-19 chemistry when the reaction was heated to 90 °C, considerable changes appeared during radiofluorination. In the latter case, the radiochemical yields increased, and degradation of the 2-fluoro-propan-1-amine isomer (b) occurred, leading to a regiospecific reaction in the radiolabeling of [18F]-fluorodeprenyl. This method involving nucleophilic radiofluorination at RT was successfully applied to the radiolabeling of [18F]-2-fluoroethylamines in which the influence of the N-substituent was also observed.
- Médoc, Marie,Sobrio, Franck
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p. 10086 - 10097
(2015/11/03)
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- C-F bond substitution via aziridinium ion intermediates
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Aliphatic 1,2-aminofluorides undergo extremely fast substitution reactions under the influence of lanthanum tris(hexamethyldisilazide). The substitution proceeds via an in situ generated aziridinium ion intermediate, which subsequently undergoes ring opening by addition of a nucleophile, yielding various β-substituted amines.
- Tr?ff,Janjetovic,Hilmersson
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p. 13260 - 13263
(2015/08/24)
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- Comprehensive evaluation of the physicochemical properties of Ln III complexes of aminoethyl-DO3A as pH-responsive T1-MRI contrast agents
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N-Substituted aminoethyl groups were attached to 1,4,7,10- tetraazacyclododecane-1,4,7-triacetic acid (DO3A) with the aim to design pH-responsive LnIII complexes based on the pH-dependent on/off ligation of the amine nitrogen to the metal ion. The following ligands were synthesized: AE-DO3A (aminoethyl-DO3A), MAE-DO3A (N-methylaminoethyl-DO3A), DMAE-DO3A (N,N-dimethylaminoethyl-DO3A) and MEM-AE-DO3A (N-methoxyethyl-N- methylaminoethyl-DO3A). The physicochemical properties of the LnIII complexes were investigated for the evaluation of their potential applicability as magnetic resonance imaging (MRI) contrast agents. In particular, a 1H and 17ONMR relaxometric study was carried out for these GdIII complexes at two different pH values: at basic pH (pendant amino group coordinated to the metal centre) and at acidic pH (protonated amine, not interacting with the metal ion). EuIII complexes allow one to estimate the number of inner-sphere water molecules through luminescence lifetime measurements and obtain some structural information through variable-temperature (VT) high-resolution 1HNMR studies. Equilibria between differently hydrated species were found for most of the complexes at both acidic and basic pH. The thermodynamic stability of CaII, ZnII, CuII and LnIII complexes and kinetics of formation and dissociation reactions of LnIII complexes of AE-DO3A and DMAE-DO3A were investigated showing stabilities comparable to currently approved GdIII-based CAs. In detail, higher total basicity (Σlog KiH) and higher stability constants of Ln III complexes were found for AE-DO3A with respect to DMAE-DO3A (i.e., log KGd-AE-DO3A=22.40 and log KGd-DMAE-DO3A=20.56). The transmetallation reactions of GdIII complexes are very slow (Gd-AE-DO3A: t1/2=2.7×104h; Gd-DMAE-DO3A: 1.1×105h at pH7.4 and 298K) and occur through proton-assisted dissociation. pH Switches: N-Substituted aminoethyl-1,4,7,10- tetraazacyclododecane-1,4,7-triacetic acid (DO3A)-based complexes were prepared to obtain pH-sensitive T1-MRI contrast agents. A detailed evaluation of the physicochemical properties of LnIII complexes was undertaken by different techniques, highlighting the structural variations triggered by the protonation of the pendant amine and the effect of the substituents on the corresponding nitrogen atom (see figure).
- Baranyai, Zsolt,Rolla, Gabriele A.,Negri, Roberto,Forgacs, Attila,Giovenzana, Giovanni B.,Tei, Lorenzo
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supporting information
p. 2933 - 2944
(2014/03/21)
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- Synthesis of a new class of bis(thiourea)hydrazide pseudopeptides as potential inhibitors of β-sheet aggregation
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The modular synthesis of a novel pseudopeptide scaffold based on a bis(thiourea)hydrazide motif is reported. This compound class is designed to display "amphifinity", i.e. association with a peptide strand on one but not the other face of the scaffold, and hence could potentially inhibit β-sheet aggregation.
- Klein, Jan J.,Hecht, Stefan
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supporting information; experimental part
p. 330 - 333
(2012/02/04)
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- BISPHOSPHONATE COMPOUNDS
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Novel bisphosphonate cyclic acetal compounds are disclosed, as well as methods of preparing the compounds, pharmaceutical compositions including the compounds, and administration of the compounds in methods of treating bone metabolism disorders, such as abnormal calcium and phosphate metabolism.
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Page/Page column 68-69
(2011/05/05)
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- A selective high performance liquid chromatographic method to follow the hydrolytic degradation of nicardipine hydrochloride
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A simple, stability indicating, reverse phase high performance liquid chromatographic method was developed and validated for determination of nicardipine hydrochloride (NC) in the presence of its degradation products. The chromatographic separation was performed on Hypersil, BDS-C18, 30 cm × 3.9 mm id, at ambient temperature with UV-detection at 254 nm. A mixture of 20% (v/v) aqueous 0.01 M sodium acetate/acetic acid buffer (pH 4.5) and 80% acetonitrile was used as the mobile phase at a flow rate of 1.5 mL min-1, losartan was used as internal standard. The calibration curve is linear over the concentration range 5-40 μg mL-1, with a regression coefficient of 0.9984 and the % recovery was 99.78±0.17. The method was used to investigate the kinetics of alkaline, acids induced degradation, effect of buffer concentration and temperature. The degradation followed first-order kinetics. The rate constant, half-life time, and activation energy were calculated.
- Ibrahim,Al-Ashban,Babiker
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experimental part
p. 85 - 92
(2011/01/03)
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- A new one-pot, four-component synthesis of 1,2-amino alcohols: TiCl 3/t-BuOOH-mediated radical hydroxymethylation of imines
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(Chemical Equation Presented) An amine, an aldehyde, and methanol can be readily assembled in one pot under very mild conditions through a free-radical multicomponent reaction by using an aqueous acidic TiCl3/t-BuOOH system to afford 1,2-amino alcohols in fair to excellent yields.
- Clerici, Angelo,Ghilardi, Alessandra,Pastori, Nadia,Punta, Carlo,Porta, Ombretta
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supporting information; experimental part
p. 5063 - 5066
(2009/05/31)
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- An efficient optical resolution of nitrogen-centered chiral β-hydroxy-tetraalkylammonium salts via complexation with (R)-BINOL
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The optical resolution of nitrogen-centered chiral β-hydroxy-tetraalkylammonium bromides is demonstrated by using chiral BINOL as a complexing agent. Determination of the enantiopurities and absolute configurations of the resolved N-chiral tetraalkylammonium salts are described.
- Tayama, Eiji,Tanaka, Hiroyuki
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p. 4183 - 4185
(2008/02/05)
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- Synthesis of 2,4,6-tri-substituted-1,3,5-triazines
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Several specific synthetic protocols were developed for the preparation from cyanuric chloride of a range of symmetric and non-symmetric di- and tri-substituted 1,3,5-triazines containing alkyl, aromatic, hindered, chiral and achiral hydroxyalkyl, ester and imidazole groups via sequential nucleophilic substitution of the C-Cl bond by C-O, C-N and C-S bonds.
- Afonso, Carlos A. M.,Lourenco, Nuno M. T.,De Rosatella, Andreia A.
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- Synthesis of N-(dialkylaminoalkyl)alcohols by homogeneously catalyzed hydrogenolysis of cyclic N,O-acetals
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The homogeneously catalyzed hydrogenation of 1,3-oxazolidines affording unsymmetrically substituted 2-N-(dialkylamino)ethanols is reported showing for the first time that Rh(I) catalysts based on chelating diphosphines can be advantageous for this reaction.
- Tararov, Vitali I.,Kadyrov, Renat,Riermeier, Thomas H.,B?rner, Armin
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p. 375 - 380
(2007/10/03)
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- NPY antagonists: spiroisoquinolinone derivatives
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A series of non-peptidergic antagonists of NPY have been synthesized and are comprised of spiroisoquinolinone derivatives of Formula I. As antagonists of NPY-induced feeding behavior, these compounds and known analogs are expected to act as effective anorexiant agents in promoting weight loss and treating eating disorders.
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Page column 12
(2008/06/13)
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- Control of aminophosphine chelate ring-opening in Pt(II) and Pd(II) complexes: Potential dual-mode anticancer agents
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We show that bis(aminophosphine) complexes of the type [M(R1R2N(CH2)nPPh2)2 ]2+, M = Pt(II) or Pd(II), can exist in chelate ring-closed and ring-opened forms both in the solid state and in aqueous solution. The equilibrium between them in solution can be controlled by the nature of the groups R1 and R2 (H, Me, Bz, cyclohexyl), by the bridge length n, and by the pH and Cl- concentration. X-Ray crystal structures are reported for the ring-closed complexes cis-[Pt(H2N(CH2)2PPh2-P,N)2 ]Cl2, cis-[Pt(H2N(CH2)3PPh2-P,N)2 ]Cl2, and cis-[Pt(Me(H)N(CH2)2PPh2-P,N)2][HCl 2]2, the mono-ring-opened complex cis-[Pd(Me2N(CH2)2PPh2-N,P)Cl(Me 2NH(CH2)2PPh2-P)](NO3) 2, the di-ring-opened complex cis-[Pt(Me2N(CH2)3PPh2-P)2 CL2], and, for comparison, the monochelate cis-[Pd(Me2N(CH2)3PPh2-N,P)CL2 ]. These square-planar complexes exhibit varying degrees of distortion and variable M-N bond lengths dependent not only on the trans influence of P but also on steric effects within the complex, pH-induced chelate ring-opening of cis-[Pt(Me2N(CH2)2PPh2-P,N)2 ]CL2 had an associated pK value of 6.9. In contrast, complexes with R1 and R2 = H, n = 2 or 3 or R1 = H and R2 = Me, n = 2, are more difficult to ring-open. Thus the complexes cis-[Pt(Me(H)N(CH2)2-PPh2-P,N)2]CL 2 and cis-[Pt(H2N(CH2)3PPh2-P,N)2 ]CL2, had associated pK values of 2.1 and 2.9, respectively. These aminophosphine complexes may exhibit anticancer activity by two mechanisms: by disrupting mitochondrial membrane potentials as bis-chelated (ring-closed) lipophilic cations, or by direct binding to DNA bases as ring-opened complexes.
- Habtemanam, Abraha,Watchman, Beth,Potter, Brian S.,Palmer, Rex,Parsons, Simon,Parkin, Andrew,Sadler, Peter J.
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p. 1306 - 1318
(2007/10/03)
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- Generation and reactivity of α-amino-substituted arylmethyllithium organometallics
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Reductive cleavage of open chain and cyclic α-N,N-dialkylamino- substituted benzyl alkyl ethers 1a-f with a dispersion of Li metal and a catalytic amount of naphthalene in THF, allowed easy access to a wide array of α-N,N-dialkylamino-substituted benzyllithium derivatives. Reaction of these organometallics with various electrophiles afforded the expected products in satisfactory yields. (C) 2000 Elsevier Science Ltd.
- Azzena, Ugo,Pilo, Luciano,Piras, Elisabetta
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p. 3775 - 3780
(2007/10/03)
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- Compounds having antidiabetic, hypolipidemic, antihypertensive properties, process for their preparation and pharmaceutical compositions containing them
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Thiazolidinediones of formula (I) their tautomeric forms, their derivatives, their stereoisomers, their polymorphs, their pharmaceutically acceptable salts, their pharmaceutically acceptable solvates and pharmaceutical compositions containing them having antidiabetic, hypolipidemic, and antihypertensive properties have been prepared. STR1
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- Design and synthesis of imidazoline derivatives active on glucose homeostasis in a rat model of type ii diabetes. 2. Syntheses and biological activities of 1,4-dialkyl-, 1,4-dibenzyl, and 1-benzyl-4-alkyl-2-(4',5'- dihydro-1'H-imidazol-2'-yl)piperazines and isosteric analogues of imidazoline
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Piperazine derivatives have been identified as new antidiabetic compounds. Structure-activity relationship studies in a series of 1-benzyl- 4-alkyl-2-(4',5'-dihydro-1'H-imidazol-2'-yl)piperazines resulted in the identification of 1-methyl-4-(2',4'-dichlorobenzyl)-2-(4',5'-dihydro-1'H- imidazol-2'-yl)piperazine, PMS 812 (S-21663), as a highly potent antidiabetic agent on a rat model of diabetes, mediated by an important increase of insulin secretion independently of α2 adrenoceptor blockage. These studies were extended to find additional compounds in these series with improved properties. In such a way, substitution of both piperazine N atoms was first optimized by using various alkyl, branched or not, and benzyl groups. Second, some modifications of the imidazoline ring and its replacement by isosteric heterocycles were carried out, proceeding from PMS 812, to evaluate their influence on the antidiabetic activity. The importance of the distance between the imidazoline ring and the piperazine skeleton was studied third. Finally, the influence of the N-benzyl moiety was also analyzed compared to a direct N-phenyl substitution. The pharmacological evaluation was performed in vivo using glucose tolerance tests on a rat model of type II diabetes. The most active compounds were 1,4-diisopropyl-2-(4',5'-dihydro-1'H-imidazol-2'- yl)piperazine (41a), PMS 847 (S-22068), and 1,4-diisobutyl-2-(4',5'-dihydro- 1'H-imidazol-2'-yl)piperazine (41b), PMS 889 (S-22575), which strongly improved glucose tolerance without any side event or hypoglycemic effect. More particularly, PMS 847 proved to be as potent after po (100 μmol/kg) as after ip administration and appears as a good candidate for clinical investigations.
- Le Bihan, Ga?lle,Rondu, Frédéric,Pelé-Tounian, Agnès,Wang, Xuan,Lidy, Sandrine,Touboul, Estéra,Lamouri, Aazdine,Dive, Georges,Huet, Jack,Pfeiffer, Bruno,Renard, Pierre,Guardiola-Lema?tre, Béatrice,Manéchez, Dominique,Pénicaud, Luc,Ktorza, Alain,Godfroid, Jean-Jacques
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p. 1587 - 1603
(2007/10/03)
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- Thiazolidinedione derivatives having antidiabetic, hypolipidaemic antihypertensive properties, process for their preparation and pharmaceutical compositions containing them
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A compound of the general formula (I), where A represents, substituted or unsunstituted unsaturated aliphatic, alicyclic, aromatic, heterocyclic groups, B represents a substituted or unsubstituted divalent alkylene or alkenyl group having 1 to 10 carbon atoms, wherein substituents may be present in one or more of the divalent alkylene or alkenyl groups, D represents a substituted or insubstituted divalent alkenyl, alkynyl, aralkyl alkoxycarbonyl or aryloxycarbonyl groups, X represents CH2, C=O, CH-OH, sulphur, oxygen, N-Y, where Y represents hydrogen, substituted or unsubstituted alkyl, aryl, aralkyl or acyl, Ar represents a divalent aromatic, single or fused ring system, with or without substituents, the ring may contain one or more hetero atoms selected from nitrogen, sulphur, or oxygen; R1and R2each represents hydrogen or together represent a bond either or both may be substituents or both together form a part of a ring. Methods for preparing the compound and pharmaceutical compositions containing a compound of formula (I).
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- Novel 2-amino-1,4-dihydropyridine calcium antagonists. I. Synthesis and antihypertensive effects of 2-amino-1,4-dihydropyridine derivatives having nitroxyalkoxycarbonyl groups at 3- and/or 5-position
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Novel 2-amino-1,4-dihydropyridine derivatives, which contain nitroxy-alkoxycarbonyl groups at the 3- and/or 5-position, were synthesized and their pharmaceutical effect was evaluated in spontaneously hypertensive rats. The structure-activity relationships are discussed in terms of potency, onset-rapidity, and duration of antihypertensive activity. Remarkably prolonged duration of antihypertensive action was observed when a tertiary amino group was introduced on either side of an ester chain.
- Kobayashi,Inoue,Kita,Yoshiya,Nishino,Oizumi,Kimura
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p. 788 - 796
(2007/10/02)
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- Novel 2-amino-1,4-dihydropyridine calcium antagonists. II. Synthesis and antihypertensive effects of 2-amino-1,4-dihydropyridine derivatives having N,N-dialkylaminoalkoxycarbonyl groups at 3- and/or 5-positions
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Novel 2-amino-1,4-dihydropyridine derivatives I, which contain N,N-dialkylaminoalkoxycarbonyl groups at the 3- and/or 5-position, were synthesized and their antihypertensive effects were evaluated in spontaneously hypertensive rats. Remarkably prolonged duration of antihypertensive action was observed when a tertiary amino group was introduced into either the 3- or 5-ester side-chain of the 1,4-dihydropyridine ring. In particular, the compounds containing cyclic amino moieties at the 3-position showed greater potency than those with acyclic amino moieties. Chemical modification studies indicated that the two ester side-chains of 1,4-dihydropyridine at the 3- and 5-position might function in a different manner in relation to the antihypertensive activities. 3-(1-Benzhydrylazetidin-3-yl) 5-isopropyl 2-amino-1,4-dihydro-6-methyl-4-(3-nitrophenyl)-3,5-pyridine-dicarboxyl ate, I-43 (CS-905), exhibited potent and long-lasting antihypertensive effects with gradual onset of action, and is a promising candidate as an antihypertensive drug.
- Kobayashi,Inoue,Nishino,Fujihara,Oizumi,Kimura
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p. 797 - 817
(2007/10/02)
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- Reductive Cleavage of N-Substituted 2-Aryl-1,3-oxazolidines: Generation of α-Amino-Substituted Carbanions
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The behavior of several N-substituted 2-aryl-1,3-oxazolidines has been investigated under conditions of electron transfer from alkali metals in aprotic solvents.The reduction led to the regioselective cleavage of the benzylic carbon-oxygen bond, with formation of the corresponding N-substituted benzylamino alcohols in good yields.Investigation of the mechanism of this reductive cleavage, with the aid of labeling experiments, showed the intermediate formation of α-tertiary amino-substituted carbanions.
- Azzena, Ugo,Melloni, Giovanni,Nigra, Cristina
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p. 6707 - 6711
(2007/10/02)
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- TRIMETHYLSILYLDIAZOMETHANE: A CONVENIENT REAGENT FOR THE O-METHYLATION OF ALCOHOLS
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Trimethylsilyldiazomethane smoothly reacts with alcohols in dichloromethane in the presence of 42percent aqueous fluoroboric acid to give methyl ethers in good to high yields.
- Aoyama, Toyohiko,Shioiri, Takayuki
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p. 5507 - 5508
(2007/10/02)
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- Omega-quaternary ammonium alkyl esters and thioesters of acidic nonsteroidal antiinflammatory drugs
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Quaternary ammonium alkyl esters and thioesters of acidic nonsteroidal anti-inflammatory drugs (NSAIDs) are disclosed. These esters and thioesters display the anti--inflammatory profile of the parent NSAIDs with greatly reduced gastrointestinal irritancy, providing a more favorable separation of therapeutic activity and toxicological side effects than the parent NSAIDs.
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- Ethylenediamine derivatives and pharmaceutical compositions containing same
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New derivatives of 1,2-ethylenediamine and salts thereof endowed with vascular antispasmodic and antiallergic activity; processes for preparing them, some new intermediates useful in their preparation and pharmaceutical compositions containing them.
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- PREPARATION DE SELS D'AMINOALKYLPHOSPHONIUMS
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Three synthetic methods have been applied to prepare amino phosphonium salts: (C6H5)3P+-(CH2)n-N-.The best ways have been determined for different n values and different substituents on the nitrogen atom.In all cases, yields are better with n=3, but no intramolecular stabilization has been detected.
- Dantas, T. N. de Castro,Laval, J. P.,Lattes, A.
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