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Novel Aryl-Substituted Pyrimidones as Inhibitors of 3-Mercaptopyruvate Sulfurtransferase with Antiproliferative Efficacy in Colon Cancer
The enzyme 3-mercaptopyruvate sulfurtransferase (3-MST) is one of the more recently identified mammalian sources of H2S. A recent study identified several novel 3-MST inhibitors with micromolar potency. Among those, (2-[(4-hydroxy-6-methylpyrimidin-2-yl)sulfanyl]-1-(naphthalen-1-yl)ethan-1-one) or HMPSNE was found to be the most potent and selective. We now took the central core of this compound and modified the pyrimidone and the arylketone sides independently. A 63-compound library was synthesized; compounds were tested for H2S generation from recombinant 3-MST in vitro. Active compounds were subsequently tested to elucidate their potency and selectivity. Computer modeling studies have delineated some of the key structural features necessary for binding to the 3-MST's active site. Six novel 3-MST inhibitors were tested in cell-based assays: they exerted inhibitory effects in murine MC38 and CT26 colon cancer cell proliferation; the antiproliferative effect of the compound with the highest potency and best cell-based activity (1b) was also confirmed on the growth of MC38 tumors in mice.
Bantzi, Marina,Augsburger, Fiona,Loup, Jérémie,Berset, Yan,Vasilakaki, Sofia,Myrianthopoulos, Vassilios,Mikros, Emmanuel,Szabo, Csaba,Bochet, Christian G.
p. 6221 - 6240
(2021/05/06)

Efficient synthesis of 5-(hydroxymethyl)piperazin-2-ones using automatically prepared chiral bromocarboxylic acid and Garner's aldehyde as versatile building blocks
An efficient method for the synthesis of substituted 5-(hydroxymethyl)piperazin-2-ones was established by using an automated synthesis process. Thirteen piperazinones were synthesized from chiral α-bromocarboxylic acids and Garner's aldehyde which were prepared by using our originally developed automated synthesizer, ChemKonzert. The automated method of synthesizing chiral α-bromocarboxylic acids was efficient and safe because the rate of the dropwise addition of the reagent can be controlled using the automated synthesizer. This method is expected to contribute to the synthesis of pharmaceuticals.
Masui, Hisashi,Naito, Kohei,Minoshima, Mai,Kusayanagi, Akira,Yosugi, Sae,Shoji, Mitsuru,Takahashi, Takashi
supporting information

(2021/05/04)

Synthesis method of ethyl 3-hydroxyhexanoate
The invention discloses a synthesis method of ethyl 3-hydroxyhexanoate. The method is characterized by comprising the following steps: reacting bromine with acetic acid to prepare bromoacetic acid; reacting the bromoacetic acid with ethanol in the presence of sulfuric acid to generate ethyl bromoacetate; adding 500kg of dichloromethane and 140kg of n-butyraldehyde into a reaction kettle; adding acatalyst, heating to reflux, dropwise adding 250kg of the ethyl bromoacetate serving as a product obtained in the previous step, controlling the dropwise adding speed, controlling the adding to be completed within 3 hours in a reflux state, preserving heat for 2 hours, cooling to room temperature, washing to neutrality, transferring into a rectifying tower, and rectifying to obtain a qualified product, namely the ethyl 3-hydroxyhexanoate.
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Paragraph 0017; 0018; 0021; 0022; 0025; 0026; 0029; 0030

(2020/02/27)

1,3,4,9-TETRAHYDRO-2H-PYRIDO[3,4-B]INDOLE DERIVATIVE COMPOUNDS AND USES THEREOF
The present invention relates to 1,3,4,9-tetrahydro-2H-pyrido[3,4-b]indole derivative compounds and uses thereof. In particular, compounds of the invention have antibacterial activity and/or are capable of re-sensitizing methicillin-resistant Staphylococcus aureus to a P-lactam antibiotic or a combination of a P-lactam antibiotic and a P-lactamase inhibitor. The present invention also relates to a method for producing and using said compounds.
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Paragraph 0134-0136

(2020/03/05)

A Straightforward Homologation of Carbon Dioxide with Magnesium Carbenoids en Route to α-Halocarboxylic Acids
The homologation of carbon dioxide with stable, (enantiopure) magnesium carbenoids constitutes a valuable method for preparing α-halo acid derivatives. The tactic features a high level of chemocontrol, thus enabling the synthesis of variously functionalized analogues. The flexibility to generate magnesium carbenoids through sulfoxide-, halogen- or proton- Mg exchange accounts for the wide scope of the reaction. (Figure presented.).
Monticelli, Serena,Urban, Ernst,Langer, Thierry,Holzer, Wolfgang,Pace, Vittorio
supporting information
p. 1001 - 1006
(2019/01/30)

Reaction of Lithium Acylate α-Carbanions with Carbon Tetrabromide
Lithium acylate α-carbanions generated by metalation of acetic, butanoic, and 2-methylpropanoic acids with lithium diisopropylamide in THF under argon reacted with carbon tetrabromide at 20-25°C (2 h) to produce butanedioic acid or its 2,3-diethyl and 2,2,3,3-tetramethyl derivatives, as well as the corresponding 2-bromocarboxylic acids and bromoform. The effect of the halogen nature in carbon tetrahalide (CCl4, CBr4) on the reaction selectivity is discussed.
Zorin,Zaynashev,Zorin
p. 1527 - 1531
(2019/12/28)

Synthesis and schematic mechanism of 3-phenylamino-4-phenyl-5-tetra-O-acetyl-β-D-glucopyranosylimino-1,2,4-dithiazolidines and Its De-acetylated Nucleoside
A systematic synthesis of 3-phenylimino-4-phenyl-5-tetra-O-acetyl-β-D-glucopyranosylimino-1,2,4-dithiazolidine (acetylated glucopyranosylimino nucleoside) from glucose as starting material. The steps included acetylating glucose to glucose penta-acetate (II). Step 2 involves the bromination of glucose penta-acetate (II) to 2,3,4,6 tetra-O-acetyl-α-D-glucopyranosyl bromide (III). In step 3 compound (III) reacted with lead thiocyanate to give 2,3,4,6-tetra-O-acetyl-β-D-glucopyranosyl isothiocyanate (IV). In the step 4 N-phenyl-3-tetra-O-acetyl-β-D-glucopyranosyl isothiocyanate (V) was prepared. In the last step on refluxing compound (V) with N-phenyl S-chloro isothiocarbamoyl chloride to yield acetylated glucopyranosyl nucleoside. Furthermore de-acetylating of acetylated glucopyranosyl nucleoside was carried out to obtain 3-phenylimino-4-phenyl-5-β-D-gluopyranosyl imino 1,2,4-dithiazolidine (de-acetylated glucopyranosylimino nucleoside). The synthesized acetylated glucopyranosylimino nucleoside and deacetylated glucopyranosylimono nucleoside were structurally confirmed by elemental analysis, ultraviolet spectral analysis, infrared spectroscopy, nuclear magnetic resonance spectroscopy and mass spectroscopy.
Hardas, Aruna,Tayade, Priti
p. 2310 - 2316
(2018/09/10)

Reductive Dehalogenation of Monobromo- and Tribromoacetic Acid by Sodium Borohydride Catalyzed by Gold Nanoparticles Entrapped in Sol–Gel Matrices Follows Different Pathways
An efficient, green, and reusable system comprising gold nanoparticles entrapped in an organically modified sol–gel silica matrix was found to catalyze the reduction of monobromo- and tribromoacetic acid by NaBH4. Interestingly, the reduction of tribromoacetic acid yielded succinic acid along with acetic acid, whereas monobromoacetic acid was reduced only to acetic acid. The relative yields of succinic acid and acetic acid depended on the rate of addition of BH4–. Slow addition resulted in the formation of succinic acid as the major product. A variable product distribution was achieved as a result of the different pathways for dehalogenation.
Adhikary, Jaydeep,Meistelman, Michael,Burg, Ariela,Shamir, Dror,Meyerstein, Dan,Albo, Yael
p. 1510 - 1515
(2017/03/31)

Reactions of α-carbanions of lithium acylates with N,N-diethyl-N-chloro- and N,N-diethyl-N-bromoamines
The interaction of α-carbanions of lithium acylates (prepared via metalation of acetic, butyric, or isobutyric acid with lithium diisopropylamide in tetrahydrofuran under argon atmosphere) with N,N-diethyl-N-chloro- or N,N-diethyl-N-bromoamine has resulte
Zorin,Zainashev,Zorin
p. 2469 - 2472
(2016/12/24)

Nucleofugality of aliphatic carboxylates in mixtures of aprotic solvents and water
The leaving group ability (nucleofugality) of fluoroacetate, chloroacetate, bromoacetate, dichloroacetate, trifluoroacetate, trichloroacetate, heptafluorobutyrate, formate, isobutyrate, and pivalate have been derived from the solvolysis rate constants of the corresponding X,Y-substituted benzhydryl carboxylates in 60 % and 80 % aqueous acetonitrile and 60 % aqueous acetone, applying the LFER equation: log k = sf(Ef + Nf). The experimental barriers (ΔG?,exp) for solvolyses of 11 reference dianisylmethyl carboxylates in these solvents correlate very well (r = 0.994 in all solvents) with ΔG?,model of the model σ-assisted heterolytic displacement reaction of cis-2,3-dihydroxycyclopropyl trans-carboxylates calculated earlier. Linear correlation observed between the log k for the reference dianisylmethyl carboxylates and the sf values enables estimation of the reaction constant (sfestim). Using the ΔG?,exp vs. ΔG?,model correlation, and taking the estimated sfestim, the nucleofugality parameters for other 34 aliphatic carboxylates have been determined in 60 % and 80 % aqueous acetonitrile and 60 % aqueous acetone. The most important variable that determines the reactivity of aliphatic carboxylates in aprotic solvent/water mixtures is the inductive effect of the group(s) attached onto the carboxylate moiety.
Mati, Mirela,Denegri, Bernard,Kronja, Olga
p. 375 - 384
(2015/10/12)

2-Iodoxybenzenesulfonic acid-catalysed oxidation of primary and secondary alcohols with oxone in cetyl trimethylammonium bromide micelles at room temperature
A mild and green protocol for alcohol oxidation using 2-iodoxybenzene sulfonic acid/oxone at room temperature in CTAB micelles has been developed. Typically, secondary benzyl alcohols were oxidised to ketones and primary benzyl alcohols to aldehydes in good yields in 2 h. Under harsher conditions (100 °C/24 h), aliphatic alcohols were oxidised to ketones or organic acids in moderate to high yields.
Liu, Yangyang,Wang, Boliang
p. 427 - 431
(2014/08/05)

Tubulisine derivatives as anticancer drugs
Tubulisine derivatives of formula (A) having a high cytotoxicity are described.
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(2011/04/18)

Rotanone Analogs: Method of Preparation and Use
The present invention provides rotenone analogs and methods of making and using them. Labeled with single photon and positron emitting isotopes, the rotenone analogs of the present invention are useful in, for example, clinical imaging applications as tracers to measure cardiac blood flow and detect regions of ischemia.
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(2009/06/27)

Ureido substituted benzoic acid compounds and their use for nonsense suppression and the treatment of disease
The invention encompasses ureido substituted benzoic acid compounds, compositions comprising the compounds and methods for treating or preventing diseases associated with nonsense mutations of mRNA by administering these compounds or compositions.
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Page/Page column 50

(2008/06/13)

Bisaryl derivatives having FSH modulatory activity
The invention relates to bisaryl derivatives of the formula I, wherein (R,R) is selected from (H,H), O, (H,CH3), (H,OH) and (H,CN); Ar is substituted phenyl and A is a group of formula II, III, IV or V: An example is (3S,6S)-1-N-(7-phenylheptyl)-3-(4-(3,4,5-trimethoxyphenyl)benzyl)-4-N-methyl-6-methyl-2,5-dioxo-1,4-piperazine: The compounds of the invention have FSH receptor modulatory activity and can be used for the control of fertility, for contraception or for treatment of hormone-dependent disorders.
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(2008/06/13)

Preparation and Characterization of [5-13C]-(2S,4R)-Leucine and [4-13C]-(2S,3S)-Valine - Establishing Synthetic Schemes to Prepare Any Site-Directed Isotopomer of L-Leucine, L-Isoleucine and L-Valine
In this paper a chemo-enzymatic method has been developed that gives access to any isotopomer of the essential amino acids isoleucine and valine. The method gives the correct introduction of the second chiral center in (2S,3S)-isoleucine and allows for discrimination between the two prochiral methyl groups in valine as shown by the preparation of (2S,3S)-[4- 13C] valine. For the preparation of (2S)-leucine in any isotopomeric form, the O'Donnell method to prepare optically active amino acids has been used. The protected glycine scaffold used in this method has been prepared by a strategy that allows access to any isotopomeric form. The preparation of [5-13C]-(2S,4R)-leucine shows that the O'Donnell method in combination with the Evans method to obtain chiral 2-methylpropyl iodide leads to a good discrimination between the two prochiral methyl groups. The O'Donnell strategy for the preparation of α-amino acids is preferred over other methods since the reaction conditions are mild, the chiral auxiliary can be easily recovered and the optically active product can be easily separated. For the preparation of isotopically enriched valine and isoleucine the O'Donnell method is not suitable, because the alkyl substituents involved have a secondary halide substituent which is sterically too hindered to give an effective reaction with the protected glycine. Wiley-VCH Verlag GmbH & Co. KGaA, 69451 Weinheim, Germany, 2003.
Siebum, Arjan H. G.,Woo, Wei Sein,Lugtenburg, Johan
p. 4664 - 4678
(2007/10/03)

Compounds for altering mitochondrial function and cellular responses
Compounds for treating diseases by altering mitochondrial function that affects cellular processes, as well as to compositions and methods related thereto. The compounds have the structure wherein R1, R2, R3 and A are as defined herein.
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(2008/06/13)

Isoquinoline derivatives and isoquinoline combinatorial libraries
The present invention provides the synthesis of heterocyclic compounds based on the isoquinoline ring. More specifically, the invention provides novel isoquinoline derivatives as well as novel libraries comprised of such compounds.
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(2008/06/13)

4-unsubstituted dihydroisoquinolinone derivatives and combinatorial libraries thereof
The present invention relates to novel dihydroisoquinolinone (DHQ) derivative compounds of the following formula: wherein R1to R7, X, Y, Z, b, c and d have the meanings provided herein. The invention further relates to combinatorial libraries containing two or more such compounds, as well as methods of preparing DHQ derivative compounds.
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(2008/06/13)

Mapping the substrate selectivity of new hydrolases using colorimetric screening: Lipases from Bacillus thermocatenulatus and Ophiostoma piliferum, esterases from Pseudomonas fluorescens and Streptomyces diastatochromogenes
Recent advances in biochemistry and molecular biology have simplified the discovery and preparation of new hydrolases. Although these hydrolases might solve problems in organic synthesis, measuring their selectivity, especially enantioselectivity, remains tedious and time consuming. Recently, we developed a colorimetric screening method to measure the enantioselectivity of hydrolases. Here we apply this rapid screening method to map the substrate selectivity of four new hydrolases: lipases from the thermophilic Bacillus thermocatenulatus (DSM 730, BTL2) and a filamentous fungus Ophiostoma piliferum (NRRL 18917, OPL) and esterases from two bacteria, Pseudomonas fluorescens (SIK-W1, esterase I, PFE) and Streptomyces diastatochromogenes (Tue 20, SDE). We screened a general library of 29 substrates and a chiral library of 23 pairs of enantiomers. All four hydrolases catalysed the hydrolysis of unnatural substrates, but the two lipases accepted a broader range of substrates than the two esterases. As expected, the two lipases favoured more hydrophobic substrates, while the two esterases showed a preference for smaller substrates. Several moderately enantioselective reactions were identified for the solketal esters: BTL2, butyrate, E = 7.9 (R); octanoate, E = 4.9 (R) and 3-bromo-2-methyl propionate methyl esters, PFE, E = 12 (S); SDE, E = 5.6 (S). OPL showed low enantioselectivity toward all substrates tested. The current colorimetric screen could not measure the selectivity for several slow-reacting substrates. Traditional screening identified high enantioselectivity of BTL2 and PFE toward one of these slow substrates, 1-phenylethyl acetate (E>50).
Liu, Andrew Man Fai,Somers, Neil A.,Kazlauskas, Romas J.,Brush, Terry S.,Zocher, Frank,Enzelberger, Markus M.,Bornscheuer, Uwe T.,Horsman, Geoff P.,Mezzetti, Alessandra,Schmidt-Dannert, Claudia,Schmid, Rolf D.
p. 545 - 556
(2007/10/03)

Reduction of haloacetic acids by Fe0: Implications for treatment and fate
To predict the fate of haloacetic acids (HAAs) in natural or engineered systems, information is needed concerning the types of reactions that these compounds undergo, the rates of those reactions, and the products that are formed. Given that many drinking water distribution systems consist of unlined cast iron pipe, reactions of HAAs with elemental iron (Fe0) may play a role in determining the fate of HAAs in these systems. In addition, zerovalent iron may prove to be an effective treatment technology for the removal of HAAs from chlorinated drinking water and wastewater. Thus, batch experiments were used to investigate reactions of four trihaloacetic acids, trichloroacetic acid (TCAA), tribromoacetic acid (TBAA), chlorodibromoacetic acid (CDBAA), and bromodichloroacetic acid (BDCAA), with Fe0. All compounds readily reacted with Fe0, and investigation of product formation and subsequent disappearance revealed that the reactions proceeded via sequential hydrogenolysis. Bromine was preferentially removed over chlorine, and TBAA was the only compound completely dehalogenated to acetic acid. In compounds containing chlorine, the final product of reactions with Fe0 was monochloroacetic acid. Halogen mass balances were 95-112%, and carbon mass balances were 62.6-112%. The pseudo-first-order rate constants for trihaloacetic acid degradation were as follows: BDCAA (10.6 ± 3.1 h-1) > CDBAA (1.43 ± 0.32 h-1) ≈ TBAA (1.41 ± 0.28 h--1) ? TCAA (0.08 ± 0.02 h-1).
Hozalski, Raymond M.,Zhang, Li,Arnold, William A.
p. 2258 - 2263
(2007/10/03)

Urokinase receptor ligands
Compounds of the invention inhibit urokinase plasminogen activator or uPAR: STR1 where R10 is --CH(R9)XCH(R1)(R11) or a capping group, where X is NR12, CR12 R15, O, S, SR12, or SR12 R15 ; R1, R9, R11, R12 R15 are each H, lower alkyl, lower alkenyl, lower alkynyl, aryl, aralkyl, aryl-alkenyl, aryl-alkynyl, aryl-cycloalkyl, substituted with 0-3 halo, OH, NH2, lower alkyl, halo-lower alkyl, lower alkoxy, lower alkylamino, lower alkylthio, CN or NO2 ; R16 is --CH(R5)C(=O)NH2, H, lower alkyl, cycloalkyl, or lower alkenyl; R2 is aryl or aralkyl, unsubstituted or substituted with 1-3 halo, OH, NH2, CN, NO2, lower alkyl, halo-lower alkyl, lower alkoxy, lower alkylamino, lower alkylthio, or cycloalkyl; R3 and R5 are each independently H or lower alkyl; R4 is --CH2 C(=O)NR13 R14, where R13 is H, lower alkyl, phenyl or benzyl, and R14 is H, aryl, or aralkyl, where R6 and R7 are each independently H, OH, NH2, CN, NO2, lower alkyl, halo-lower alkyl, lower alkoxy, lower alkylamino, lower alkylthio, or cycloalkyl, and n and m are each independently an integer from 1 to 3; and pharmaceutically acceptable acid addition salts thereof.
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(2008/06/13)

Procedure for the manufacture of 3-amino-2-oxo-pyrrolidines, new intermediates and their use
The invention is directed to a process for the preparation of lactams of Formula I. It is further directed to new advantageous intermediates of Formula II and the use thereof. By the cyclization of compounds of Formula II, compounds of Formula I are obtained.
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(2008/06/13)

Design and synthesis of potent thiol-based inhibitors of endothelin converting enzyme-1
Through directed screening of compounds prepared as metalloprotease inhibitors a compound, CGS 30084, that had potent endothelin converting enzyme-1 (ECE-1) in vitro inhibitory activity (IC50=77nM) was identified. Herein we report the synthesis and optimization of ECE-1 inhibitory activity of additional analogues from this lead. Compound 3c, the thioacetate methyl ester derivative of compound 4c, was found to be a long acting inhibitor of ECE-1 activity in rats after oral administration. (C) 2000 Elsevier Science Ltd.
Fink, Cynthia A.,Moskal, Michael,Firooznia, Fariborz,Hoyer, Denton,Symonsbergen, David,Wei, Dongchu,Qiao, Ying,Savage, Paula,Beil, Michael E.,Trapani, Angelo J.,Jeng, Arco Y.
p. 2037 - 2039
(2007/10/03)

Kinetic study of the Ce(III)-, Mn(II)-, or ferroin-catalyzed Belousov-Zhabotinsky reaction with pyruvic acid
Ce(III)-, Mn(II)-, or ferroin (Fe(phen)32+)-catalyzed reaction of bromate ion and pyruvic acid (PA) or its dimer exhibits oscillatory behavior. Both the open-chain dimer (parapyruvic acid, γ-methyl-γ-hydroxyl-α-keto-glutaric acid, DP
Lin, Hsing-Lien,Yu, Yueh-O,Jwo, Jing-Jer
p. 408 - 418
(2007/10/03)

Formation of the haloacetic acids during ozonation and chlorination of water in warsaw waterworks (Poland)
The results of the study of the HAAs formation in Water Works in Warsaw, Poland are presented. Water taken from Zegrzynskie Lake is characterized by elevated content of humic substances and algae bloom in hot seasons. The water is ozonated and chlorinated
Dojlido, Jan,Zbiec, Edward,Swietlik, Ryszard
p. 3111 - 3118
(2007/10/03)

Specific isotope enrichment of methyl methacrylate
A synthetic scheme has been developed to prepare methyl methacrylate specifically 13C-labelled at all different positions and in any combination of positions, from simple, commercially available starting materials. According to this scheme methyl (1-13C) and methyl (2-13C)methacrylate (1a and 1b) have been prepared with high label incorporation (99%).
Werkhoven, Thekla M.,Van Nispen, Reinier,Lugtenburg, Johan
p. 2909 - 2914
(2007/10/03)

Macrocyclic tetraazacyclododecane conjugates and their use as diagnostic and therapeutic agents
A group conjugates having a functionalized polyaminocarboxylate chelant that form complexes with rare earth-type metal ions, covalently attached to an antibody or antibody fragment, can be used for therapeutic and/or diagnostic purposes.
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(2008/06/13)

A simple and efficient method of preparing α-bromo carboxylic acids
A new and convenient method for α-bromination of aliphatic carboxylic acids is reported. Heating carboxylic acids for 16 hours at 85 °C in trifluoroacetic acid with 1.5 equivalents of N-bromosuccinimide and a catalytic amount of concentrated H2SO4 leads to good yields of the respective α-bromocarboxylic acids.
Zhang, Lian Hao,Duan, Jianxin,Xu, Yuelian,Dolbier Jr., William R.
p. 9621 - 9622
(2007/10/03)

Preparation of optically active α-(hydroxyphenoxy)alkanecarboxylic acids and derivatives thereof
Optically active α-(hydroxyphenoxy)-alkanecarboxylic acids or derivatives thereof, for example D-2-(4-hydroxyphenoxy)propionic acid or lower alkyl ester thereof, are prepared by (a) saponifying an alkyl ester of an optically active α-halogeno-alkanecarboxylic acid, in an alcoholic solvent medium, by reacting same with an aqueous solution of an alkali metal hydroxide, thereby providing a solution of an alkali metal salt of an optically active α-halogeno-alkanecarboxylic acid, (b) next reacting the step (a) solution thus provided with a dihydroxybenzene or salt thereof, in the presence of an alkali metal hydroxide and in an alcoholic solvent medium, and thence (c) recovering the optically active α-(hydroxyphenoxy)-alkanecarboxylic acid or derivative thereof from the medium of reaction.
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(2008/06/13)

Reactions of nucleophilic substitution involving solid organic halogen compounds under shear deformation at high pressure
Under conditions of shear deformation and high pressures (SD + HP), reactions of nucleophilic substitution were studied: 1) the replacement of aliphatic halogen atom with alkaline metal halides (halo-substituted aliphatic carboxylic acids, 1-bromoadamantane); 2) the replacement of halogen atom in aromatic nucleus (halobenzoic acids, dihalobenzenes) with halogen of salt; 3) the replacement of aliphatic halogen with hydroxyl (hydrolysis in a solid phase); 4) the replacement of halogen with amino group under deformation of the samples of ammonium α-halocarboxylates to give the corresponding amino acids.It was found that the exchange of the halogen atoms bonded with aliphatic carbon is most intensive in the mixtures of alkaline metal iodides with bromo-substituted acetic acid and propionic acids: the exchange reaction in these mixtures is observed even during grinding in the mortar. Unlike the liquid phase, under conditions of SD + HP exchange of the halogen atom of the aromatic nucleus with alkaline metal halides, proceeds successfully, and the reactivity of halides increases in the series Na K Rb Cs.Under SD + HP, 1-Br-adamantane reacts with water to form 1-adamantanol.A high reactivity of the water adsorbed by the reagents is observed. - Key words: shear deformation, high pressure, halogen derivatives of carboxylic acids, dihalobenzenes, alkaline metal halides, ammonium salts of halogen derivatives of carboxylic acids, amino acids, halo-substituted adamantanes, adamantanol, nucleophilic substitution reaction, hydrolysis, ball mill.
Zharov, A. A.,Chistotina, N. P.,Gaziev, R. G.,Yakovleva, I. I.
p. 1050 - 1055
(2007/10/02)

Complexing agents and targeting radioactive immunoreagents useful in therapeutic and diagnostic imaging compositions and methods
A targeting radioactive immunoreagent comprising a compound having the structure STR1
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(2008/06/13)

HETEROCYCLIC HYDRAZIDE DERIVATIVES OF MONOCYCLIC BETA-LACTAM ANTIBIOTICS
Antibacterial activity has been found in compounds of the formula. Compounds having the formula and pharmaceutically acceptable salts thereof, wherein: A is a bond or alkylene; Q completes a 5- or 6-membered saturated or unsaturated(including aromatic) heterocyclic ring having one or two, hetero atoms in the ring selected from nitrogen sulfur or oxygen; X is attached to an available carbon atom in the heterocyclic ring and is hydrogen or oxo; Y is attached to an available carbon atom in the heterocyclic ring and is hydrogen, amino, hydroxyl, halogen, carboxamide, nitrile, or carboxyl, except that Y is not carboxyl when the bicyclic ring completed by Q is 2-quinolyl, 3-quinolyl, or quinoxalyl; and the remaining symbols are as defined in the specification
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(2008/06/13)

Method for removing the protecting group for hydroxy group
A method for removing tri-substituted silyl group from β-lactam compound having a tri-substituted silyl group-protecting hydroxy group, which comprises treating with an acid and a fluoride selected from alkali metal fluoride, alkaline earth metal fluoride and hydrogenfluoride of organic or inorganic amine, by which the tri-substituted silyl group can be easily and effectively removed under moderate conditions so that the desired compound can be obtained in high yield at low cost.
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(2008/06/13)

Amplifier molecules for enhancement of diagnosis and therapy
Disclosed are amplifier molecules: various organic compounds having branched structures terminating with amine groups to which pharmacologically active groups can be chemically attached. A number of MRI contrast-enhancing agents were synthesized, each comprising plural active groups, such as stable nitroxides and complexes of trivalent metal cations. Such syntheses were successfully performed using a number of amplifiers having different branched structures, demonstrating the general utility of the pertinent chemistry in the synthesis of amplifiers having any of a wide variety of pharmacologically active groups. Amplifiers were also synthesized having linkers terminating with chemically reactive groups such as isothiocyanates, which render the amplifier bifunctional: attachable to polymers, biomacromolecules, or other biocompatible entity possessing multiple reactive sites such as terminal amines. Via such chemistry, the amplifiers are attachable to monoclonal antibodies for concentration of pharmacologically active groups at a desired site in the body.
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(2008/06/13)

Macrocyclic chelating agents and chelates thereof
Macrocyclic derivatives of 1,4,7,10-tetraazacyclododecane of general formula (I) hereinbelow, wherein A is a group of formula (II) hereinbelow, in which R is H or alkyl or optionally substituted benzyl or a H(OCH2 CH2)1-4-, Me(OCH2 CH2)1-4-, or Et(OCH2 CH2)1-4- group, X or O--R1, in which R1 is H or alkyl, hydroxyalkyl, alkoxyalkyl, alkoxyhydroxyalkyl or a polyoxaalkyl group or X is --NR2 R3, in which R2 and R3 are H or alkyl, hydroxyalkyl, alkoxyalkyl or alkoxyhydroxyalkyl, and B1, B2 and B3 have the same meanings as A or are H or a group of formula (III) hereinbelow, in which R4 is H or alkyl, Y is a O--R5 group, wherein R5 is H or alkyl, hydroxyalkyl, alkoxyalkyl, alkoxyhydroxyalkyl or a polyoxaalkyl group, or Y is a --NR6 R7 group, wherein R6 and R7 are H or alkyl, hydroxyalkyl, alkoxyalkyl, or alkoxyhydroxyalkyl, said derivatives optionally being salified, and the complex salts thereof, are used as pharmaceuticals and/or diagnostic agents. STR1
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(2008/06/13)

Specific esterase activity of subtilisin toward esters of α-haloacids
Esters of α-haloacids are specific substrates for subtilisin which catalyses their hydrolysis in aqueous media. The same esters undergo transesterifications in organic solvents in the presence of subtilisin immobilized on an alumina-phosphate complex.
Pugniere,Juan, C. San,Previero
p. 4883 - 4886
(2007/10/02)

Degradation of Lactic Acid and Pyruvic Acid in Belousov-Zhabotinskii Reactions
The temporal degradation of the Belousev-Zhabotinskii substrates lactic acid, pyruvic acid, bromo- and dibromo pyruvic acid is investigated.The only final product of non-brominated substrates is acetic acid.From brominated educts only brominated acetic acids result.The concentrations of the stable products are determined as a function of time.The gross reactions are mainly based on simple consecutive first order reactions.For the pyruvic acid rate constants are determined. - Keywords: Belousov-Zhabotinskii Reaction, Lactid Acid, Pyruvic Acid, Bromo Pyruvic Acid
Blume, Ruediger,Wiechoczek, Dagmar,Meier, Heinrich,Wedekind, Frank
p. 598 - 608
(2007/10/02)

Macrocyclic chelating agents and chelates thereof
Macrocyclic derivatives of 1,4,7,10-tetraazacyclo-dodecane of general formula I wherein, A is a group of formula in which, R is H or alkyl or optionally substituted benzyl or a H(OCH2CH2)1 4-, Me(OCH2CH2)1 4-, or Et(OCH2CH2)1 4- group,X is O-R1, in which R1 is H or alkyl, hydroxyalkyl, alko-xyalkyl, alkoxyhydroxyalkyl or a polyoxaalkyl group or X is -NR2R3, in which R2 and R3 are H or alkyl, hydroxyalkyl, alkoxyalkyl or alkoxyhydroxyalkyl,and, B1, B2 and B3 have the same meanings as A or are H or a group of formula in which, R4 is H or alkyl, Y is a O-R5 group, wherein R5 is H or alkyl, hydroxyalkyl, alkoxyalkyl, alkoxyhydroxyalkyl or a polyoxaalkyl group, or Y is a -NR6R7 group, wherein R6 and R7 are H or alkyl, hydroxyalkyl, alkoxyalkyl or alkoxyhydroxyalkyl, said derivatives optionally being salified, and the complex salts thereof, are used as pharmaceuticals and/or diagnostic agents.
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(2008/06/13)

Phenoxyphenyl phosphinates
Novel phenoxy-, phenylthio, anilino-, benzyl-, pyridyloxy-, pyridylthio-, pyridylamino-, or pyridylmethyl-phenyl substituted phosphinates and phosphinothioates, synthesis thereof, intermediates therefore, and the use of said novel compounds for the control of weeds.
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(2008/06/13)

ANOMALOUS TRANSNITRILATION OF β-BROMOCAPROIC ACID
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Vinokurov, V. A.,Gaevoi, E. G.,Pavlova, Yu. M.,Karakhanov, R. A.
p. 2347
(2007/10/02)

MERCURATION OF 2-ALKYL-1,3-DIOXOLAN-2-YLIUM SALTS: NEW METHOD FOR THE SYNTHESIS OF α-MERCURIO CARBOXYLIC ACIDS
In the mercuration of 2-alkyl-1,3-dioxolan-2-ylium perchlorates with mercury acetate of trifluoroacetate high yileds of mono-, di-, and tri-α-mercurio derivatives of carboxylic acids wre obtained, depenging on the proportions of the reacting substrates.
Boev, V. I.,Dombrovskii, A. V.
p. 1927 - 1930
(2007/10/02)

Process for preparing cephem lactones for cephalosporin-type antibiotics
Cephem lactones of formula (1) STR1 wherein R1 is hydrogen or an organic substituent of the type appearing as the 6-substituent of penicillins or as the 7-substituent of cephalosporins are produced from corresponding 4,5-halohydrin precursors thereof by dehalogenation. Novel stereoisomers of formula (1) compounds as well as novel intermediates for cephem lactone syntheses are disclosed. The cephem lactones produced according to the invention are of utility as intermediates for cephem-type antibiotics and have antibiotic properties of their own.
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(2008/06/13)

Process for the preparation of bromoacetic acid and esters thereof
New economically valuable and convenient methods for preparing bromoacetic acid and its esters from chloroacetic acid are disclosed.
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(2008/06/13)

Anti-inflammatory sydnones
3-Alkylthioalkyl-4-optionally substituted sydnones, useful as anti-inflammatory pharmaceutical agents, are prepared.
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(2008/06/13)