- Design and synthesis of orally active dispiro 1,2,4,5-tetraoxanes; Synthetic antimalarials with superior activity to artemisinin
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The design and synthesis of dispiro- and spirotetraoxanes through acid-catalyzed cyclocondensation of bis(hydroperoxides) with ketones were investigated. Various modular synthetic methods were used to enable many different analogues to be prepared from common achiral synthetic intermediates and some of the key reactions employed include reductive amination and mixed anhydride amide coupling reactions. The synthesis of 1,2,4,5-tetraoxanes was also dependent on several factors, including the structure of the ketone or aldehyde, temperature, solvent, pH, and the equilibria between the ketone and the precursors of cyclic peroxides. The required 1,2,4,5-tetraoxane was formed by crosscondensation of the bis(hydroperoxide) and the 1,4-cyclohexanedione was obtained in low temperature. Reductive amination of the ketone with various amino compounds also produced compounds in moderate to good quantities.
- Amewu, Richard,Stachulski, Andrew V.,Ward, Stephen A.,Berry, Neil G.,Bray, Patrick G.,Davies, Jill,Labat, Gael,Vivas, Livia,O'Neill, Paul M.
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Read Online
- Mild Functionalization of Tetraoxane Derivatives via Olefin Metathesis: Compatibility of Ruthenium Alkylidene Catalysts with Peroxides
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An easy and mild functionalization method of tetraoxane derivatives via olefin metathesis is reported. This reaction offers a new method to afford fully functionalized tetraoxanes in high yields. This method is also utilized in the functionalization of bioactive compounds.
- Jana, Anupam,Grela, Karol
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Read Online
- The Silicon-Hydrogen Exchange Reaction: A Catalytic σ-Bond Metathesis Approach to the Enantioselective Synthesis of Enol Silanes
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The use of chiral enol silanes in fundamental transformations such as Mukaiyama aldol, Michael, and Mannich reactions as well as Saegusa-Ito dehydrogenations has enabled the chemical synthesis of enantiopure natural products and valuable pharmaceuticals. However, accessing these intermediates in high enantiopurity has generally required the use of either stoichiometric chiral precursors or stoichiometric chiral reagents. We now describe a catalytic approach in which strongly acidic and confined imidodiphosphorimidates (IDPi) catalyze highly enantioselective interconversions of ketones and enol silanes. These "silicon-hydrogen exchange reactions"enable access to enantiopure enol silanes via tautomerizing σ-bond metatheses, either in a deprotosilylative desymmetrization of ketones with allyl silanes as the silicon source or in a protodesilylative kinetic resolution of racemic enol silanes with a carboxylic acid as the silyl acceptor.
- Zhou, Hui,Bae, Han Yong,Leutzsch, Markus,Kennemur, Jennifer L.,Bécart, Diane,List, Benjamin
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supporting information
p. 13695 - 13700
(2020/08/24)
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- SPIRO-LACTAM NMDA RECEPTOR MODULATORS AND USES THEREOF
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Disclosed are compounds having potency in the modulation of NMDA receptor activity. Such compounds can be used in the treatment of conditions such as depression and related disorders. Orally delivered formulations and other pharmaceutically acceptable delivery forms of the compounds, including intravenous formulations, are also disclosed.
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Page/Page column 6
(2018/03/09)
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- An investigation into the role of 2,6-lutidine as an additive for the RuCl3-NaIO4 mediated oxidative cleavage of olefins to ketones
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2,6-Lutidine has been identified as a beneficial additive for the oxidative cleavage of olefins to ketones by NaIO4 in the presence of catalytic RuCl3, improving the yield and shortening the reaction times. In the absence of 2,6-lutidine reactions stalled at the diol intermediate with incomplete conversion to the desired ketones. The reaction protocol described herein also avoids the use of harmful solvents such as CCl4 and DCE and is tolerant of a range of functional groups.
- Watson, David W.,Gill, Matthew,Kemmitt, Paul,Lamont, Scott G.,Popescu, Mihai V.,Simpson, Iain
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supporting information
p. 4479 - 4482
(2018/11/23)
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- Development of Fluorinated Analogues of Perhexiline with Improved Pharmacokinetic Properties and Retained Efficacy
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We designed and synthesized perhexiline analogues that have the same therapeutic profile as the parent cardiovascular drug but lacking its metabolic liability associated with CYP2D6 metabolism. Cycloalkyl perhexiline analogues 6a-j were found to be unsuitable for further development, as they retained a pharmacokinetic profile very similar to that shown by the parent compound. Multistep synthesis of perhexiline analogues incorporating fluorine atoms onto the cyclohexyl ring(s) provided a range of different fluoroperhexiline analogues. Of these, analogues 50 (4,4-gem-difluoro) and 62 (4,4,4′,4′-tetrafluoro) were highly stable and showed greatly reduced susceptibility to CYP2D6-mediated metabolism. In vitro efficacy studies demonstrated that a number of derivatives retained acceptable potency against CPT-1. Having the best balance of properties, 50 was selected for further evaluation. Like perhexiline, it was shown to be selectively concentrated in the myocardium and, using the Langendorff model, to be effective in improving both cardiac contractility and relaxation when challenged with high fat buffer.
- Tseng, Chih-Chung,Noordali, Hannah,Sani, Monica,Madhani, Melanie,Grant, Denis M.,Frenneaux, Michael P.,Zanda, Matteo,Greig, Iain R.
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supporting information
p. 2780 - 2789
(2017/04/21)
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- Photoinduced Oxidation of Secondary Alcohols Using 4-Benzoylpyridine as an Oxidant
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Photoinduced oxidation of secondary alcohols to ketones was achieved by utilizing an equimolar amount of 4-benzoylpyridine as an oxidant. This transformation proceeds at ambient temperature and exhibits high compatibility with polar functionalities including benzoyl, silyl, and methoxymethyl alcohol protecting groups as well as tosyloxy, bromo, sulfonyl, carbamate, ester, and carboxylic acid units. The present oxidation is solely promoted by the action of organic molecules without the aid of metallic reagents. (Chemical Equation Presented).
- Kamijo, Shin,Tao, Keisuke,Takao, Go,Tonoda, Hiroshi,Murafuji, Toshihiro
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supporting information
p. 3326 - 3329
(2015/07/15)
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- FLUORO-PERHEXILINE COMPOUNDS AND THEIR THERAPEUTIC USE
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The present invention pertains generally to the field of therapeutic compounds. More specifically the present invention pertains to certain fluoro-perhexiline compounds of the following formula (also referred to herein as FPER compounds) that are useful, for example, in the treatment of disorders (e.g., diseases) including, for example, those which are known to be treated with, or known to be treatable with, perhexiline, including, for example, disorders that are ameliorated by the inhibition of carnitine palmitoyltransferase (CPT); cardiovascular disorders such as: angina pectoris; heart failure (HF); ischaemic heart disease (IHD); cardiomyopathy; cardiac dysrhythmia; stenosis of a heart valve; hypertrophic cardiomyopathy (HCM); coronary heart disease; and other disorders, for example, diabetes and cancer. The present invention also pertains to pharmaceutical compositions comprising such compounds, and the use of such compounds and compositions, for example, in therapy.
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Page/Page column 71
(2014/12/12)
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- CYCLOHEXYL OR PIPERIDINYL CARBOXAMIDE ANTIBIOTIC DERIVATIVES
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The invention relates to antibiotic cyclohexyl or piperidinyl carboximide derivatives of formula (I) wherein R1 represents hydrogen, halogen, (C1-C4)alkyl, (C1-C4)alkoxy, cyano or COOR2, R2 being (C1-C4)alkyl;one or two of U, V, W and X represent(s) N and the remaining represent each CH, or, in the case of X, may also represent CRX, RX being a halogen atom;either B represents N and A represents CH2CH2 or CH(OR3)CH2, or B represents CH or C(OR4) and A represents OCH2, CH2CH(OR5), CH(OR6)CH2, CH(OR7)CH(OR8), CH═CH or CH2CH2;each of R3, R4, R5, R6, R7, and R8 represents independently hydrogen, SO3H, PO3H2, CH2OPO3H2 or COR9, R9 being either CH2CH2COOH or such that R9—COOH is naturally occurring amino acid or dimethylaminoglycine;and to salts of such compounds of formula (I).
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Page/Page column 32-33
(2009/05/29)
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- CYCLOHEXYL OR PIPERIDINYL CARBOXAMIDE ANTIBIOTIC DERIVATIVES
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The invention relates to antibiotic cyclohexyl or piperidinyl carboxamide derivatives of formula (I) wherein R1 represents hydrogen, halogen, (C1-C4)alkyl, (C1-C4)alkoxy, cyano or COOR2, R2 being (C1-C4)alkyl; one or two of U, V, W and X represent(s) N and the remaining represent each CH, or, in the case of X, may also represent CRx, Rx being a halogen atom; either B represents N and A represents CH2CH2 or CH(OR3)CH2, or B represents CH or C(OR4) and A represents OCH2, CH2CH(OR5), CH(OR6)CH2, CH(OR7)CH(OR8), CH=CH or CH2CH2; each of R3, R4, R5, R6, R7 and R8 represents independently hydrogen, SO3H, PO3H2, CH2OPO3H2 or COR9, R9 being either CH2CH2COOH or such that R9-COOH is a naturally occurring amino acid or dimethylaminoglycine; and to salts of such compounds of formula (I).
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Page/Page column 83
(2008/06/13)
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- INDOLINE COMPOUNDS AND THEIR USE IN THE TREATMENT OF ARTERIOSCLEROSIS
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Indoline compounds, pharmaceutical compositions containing such compounds and the use of such compounds to elevate certain plasma lipid levels, including high density lipoprotein-cholesterol and to lower certain other plasma lipid levels, such as LDL-cholesterol and triglycerides and accordingly to treat diseases which are exacerbated by low levels of HDL cholesterol and/or high levels of LDL-cholesterol and triglycerides, such as atherosclerosis and cardiovascular diseases in some mammals, including humans.
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Page/Page column 59-60
(2010/10/20)
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- 1,4-SUBSTITUTED CYCLOHEXANE DERIVATIVES
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Allylic compounds represented by the formula (I) are provided, wherein each of R1 to R8, m, n, A and X are as defined in the Specification. These compounds can inhibit Rho kinase, and can find utility in repair of damaged nerves in the central and peripheral nervous system by inducing axon growth and regeneration, and in the treatment by inhibition of Rho kinase in disease states in which Rho kinase is implicated. The compounds are relatively cell permeable and pharmaceutical compositions thereof can promote neurite growth and are also useful for the prevention of cell proliferation in malignant deseases.
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Page 109; 110
(2010/02/06)
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- Bicyclic and tricyclic amines as modulators of chemokine receptor activity
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The present application describes modulators of CCR3 of formula (I): A—E—NR1—G??(I) or pharmaceutically acceptable salt forms thereof, useful for the prevention of inflammatory diseases such as asthma and other allergic diseases.
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- Quinuclidine compounds and drugs containing the same as the active ingredient
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The present invention provides an excellent squalene synthesizing enzyme inhibitor. Specifically, it provides a compound (I) represented by the following formula, a salt thereof or a hydrate of them. In which R1 represents (1) hydrogen atom or (2) hydroxyl group; HAr represents an aromatic heterocycle which may be substituted with 1 to 3 groups; Ar represents an optionally substituted aromatic ring; W represents a chain represented by (1) —CH2—CH2— which may be substituted, (2) —CH=CH— which may be substituted, (3) —C≡C—, (4) —NH—CO—, (5) —CO—NH—, (6) —NH—CH2—, (7) —CH2—NH—, (8) —CH2—CO—, (9) —CO—CH2—, (10) —NH—S(O)l—, (11) —S(O)l—NH—, (12) —CH2—S(O)— or (13) —S(O)l—CH2— (l denotes 0, 1 or 2); and X represents a chain represented by (1) a single bond, (2) an optionally substituted C1-6 alkylene chain, (3) an optionally substituted C2-6 alkenylene chain, (4) an optionally substituted C2-6 alkynylene chain, (5) a formula —Q— (wherein Q represents oxygen atom, sulfur atom, CO or N(R2) (wherein R2 represents a C1-6 alkyl group or a C1-6 alkoxy group)), (6) —NH—CO—, (7) —CO—NH—, (8) —NH—CH2—, (9) —CH2—NH—, (10) —CH2—CO—, (11) —CO—CH2—, (12) —NH—S(O)m—, (13) —S(O)m—NH—, (14) —CH2—S(O)m—, (15) —S(O)m—CH2— (wherein m denotes 0, 1 or 2) or (16) —(CH2)n—O— (wherein n denotes an integer from 1 to 6).
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- Process for producing alpha, alpha-difluorocycloalkane compound
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A method for producing an α,α-difluorocycloalkane at high purity with good efficiency, which comprises a step of treating a fluorocycloalkene with hydrogen fluoride wherein the fluorocycloalkene has one fluorine atom directly bonded to a carbon atom of carbon-carbon unsaturated double bond, more preferably, a step of directly adding the hydrogen fluoride to a reaction mixture obtained by treating the cycloalkanone with the de-oxygen fluorinating agent.
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- Spiro compounds or salts thereof and preventives/remedies for autoimmune diseases and AP-1 inhibitors containing the same
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The spiro compounds of the present invention represented by the general formula: wherein A, R2, R3, R4, R5, R6and n are as defined in the specification, exhibit an AP-1 activity inhibitory action and, based on the AP-1 inhibitory action, suppresses the expression of a wide variety of genes and are useful as an agent for treating and preventing autoimmune diseases with lessoned side reactions.
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- Design and synthesis of non-peptidic inhibitors for the Syk C-terminal SH2 domain based on structure-based in-silico screening
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Structure-based in-silico screening was carried out for the Syk C-terminal SH2 domain. Fragments that could interact with the pY or pY+1 pockets were selected by our in-silico screening. After tethering two fragments bound to these pockets, we have designed and synthesized new compounds that show favorable interaction with the pY+3 pocket. One such compound, having a cyclohexylmalonic acid moiety identified as a novel potent phosphotyrosyl mimetic, exhibited an affinity comparable to that of the monophosphorylated ligand peptide.
- Niimi,Orita,Okazawa-Igarashi,Sakashita,Kikuchi,Ball,Ichikawa,Yamagiwa,Sakamoto,Tanaka,Tsukamoto,Fujita
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p. 4737 - 4740
(2007/10/03)
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- Fluorination with aminosulfur trifluorides
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A fluorination method of oxygen and halogen sites with diaryl-, dialkoxyalkyl-, alkylalkoxyalkyl-, arylalkoxyalkyl- and cyclic aminosulfur trifluorides fluorinating reagents is disclosed.
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- Process for the preparation of cyclohexanones
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The invention relates to a process for the preparation of cyclohexanones from the corresponding phenols by partial hydrogenation, characterized in that the reaction mixture obtained by means of the hydrogenation is treated with sulfonating agents before the isolation of the cyclohexanone.
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- Substituted imidazole compounds
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Novel 1,4,5-substituted imidazole compounds and compositions for use in therapy as cytokine inhibitors.
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- Fluorination with aminosulfur trifluorides
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A fluorination method of oxygen and halogen sites with diaryl-, dialkoxyalkyl-, alkylalkoxyalkyl-, arylalkoxyalkyl- and cyclic aminosulfur trifluorides fluorinating reagents is disclosed.
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- Dicobaltoctacarbonyl-mediated deoximation
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Treatment of oxime O-acetates with Co2(CO)8 in the presence of a base, followed by H2O at room temperature efficiently afforded the parent carbonyl compounds in high yields. Direct regeneration of carbonyl functionalities from the corresponding oxime derivatives was realized by successive exposure to acetylation conditions, Co2(CO)8 in the presence of base, and H2O. In addition, N-monosubstituted hydrazone derivatives could generate the parent carbonyl compound under the above conditions.
- Mukai, Chisato,Nomura, Izumi,Kataoka, Osamu,Hanaoka, Miyoji
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p. 1872 - 1874
(2007/10/03)
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- Collision-induced dissociation study of stereospecific elimination processes of stereoisomeric phenylcyclohexanols and their derivatives upon electron ionization
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The electron ionization (EI)-induced elimination of water, methanol and acetic acid from the M+. ions of stereoisomeric 2-, 3- and 4-phenylcyclohexanols and their methyl ethers and acetates, respectively, was studied by deuteration and collision-induced dissociation (CID) techniques. The highly stereospecific elimination processes in trans-3- and -4-phenylcyclohexanols and in the corresponding methyl ethers and acetates take place with the involvement of the benzylic hydrogen atom, suggesting syn-1,3- and syn-1,4-elimination via cyclic transition states. The elimination processes from the cis-alcohols and their methyl ethers occur mainly after ring opening, and result in the formation of mixtures of product ions. The elimination processes are non-stereospecific in the stereoisomeric 2-phenyl-substituted systems, and are preceded by ring cleavage in both cis- and trans-isomers, resulting in mixtures of cyclic and acyclic product ions. All cis-2-, -3- and -4-phenylcyclohexyl acetates undergo elimination by a McLafferty-type mechanism with the abstraction of a hydrogen atom from positions 2 and/or 6. An interesting outcome of this work is that the majority of the gas-phase isomeric hydrocarbon phenyl-C6H9 radical cations, formed either by EI-induced fragmentation of stereoisomeric phenylcyclohexyl derivatives or by EI of a variety of phenyl-C6H9 isomers, retain their structural integrities. On the other hand, the CID spectra of the even-electron phenyl-C6H10+ ions produced by chemical ionization (CI)-induced fragmentation from isomeric phenylcyclohexanols and their methyl ethers and acetates are similar, indicating loss of structural information under CI in this system.
- Khaselev,Mandelbaum
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p. 819 - 835
(2007/10/03)
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- Catalytic enantioselective synthesis of a spriofused azetidinone
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A process for producing a compound of the formula STR1 comprises the following sequence of steps: STR2 wherein the various radicals are as defined in the specification.
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- Potentiating effects of β-eudesmol-related cyclohexylidene derivatives on succinylcholine-induced neuromuscular block in isolated phrenic nerve-diaphragm muscles of normal and alloxan-diabetic mice
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β-Eudesmol, a sesquiterpenoid alcohol contained in Atractylodes lancea, potentiates succinylcholine (SuCh)-induced neuromuscular blockade. The potentiating effect is greater in diabetic muscles than in normal ones. As a ligand for affinity chromatography to study the potentiating mechanism, we designed and synthesized newly β-eudesmol-related cyclohexylidene derivatives (2-(3-hydroxy-3-methylbutyl)cyclohexylidene KTE-13, 2-(3-hydroxy-3-methylbutyl)-4-cyclohexyl carboxylic acid; KTE-32 and 4-tert-butoxycarbonyl-2- (3-hydroxy-3-methylbutyl) cyclohexylidene; KTE-33). We examined the potentiating effects of those compounds in phrenic nerve-diaphragm muscle preparations of normal and alloxan-diabetic mice. KTE-33 (100 μM) potentiated more greatly SuCh-induced neuromuscular blockade in diabetic muscles than in normal ones (the potentiating ratios in normal and diabetic muscles were 6.7 and 10.6, respectively), while KTE-13 (100 μM) and -32 (200 μM) potentiated weakly. These results suggest that the ester group in KTE-33 rather than a carboxyl group in KTE-32 is important in inducing the potentiation of SuCh-induced neuromuscular blockade in diabetic state.
- Kimura,Diwan,Yanagi,Kon-No,Nojima,Kimura
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p. 407 - 410
(2007/10/03)
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- Mechanistic Studies of the Palladium(II)-Copper(II)-mediated Demercuriation of Cycloalkyl and Cycloalkylmethyl Systems
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The likely events involved in the conversion of cyclohexylmethylmercuric chloride into predominantly trans-4-methylcyclohexyl chloride, on treatment with PdCl2-CuCl2 in acetic acid, have been identified by product and deuterium-labelling studies, as well as by the behaviour of probable intermediates.Extension to related cycloalkyl- and cycloalkylmethyl--mercuric chloride is reported, and mechanistic changes as a function of ring size, with elimination-re-addition of being important in cyclohexyl systems, but carbocation formation dominating in cyclooctyl cases.
- Wells, Adam P.,Kitching, William
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p. 527 - 536
(2007/10/02)
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- Synthesis of Bridgehead-Substituted Bicycloheptanes by Radical Cyclization
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A kinetic investigation shows that the rate of cyclization (kC) of the (4-methylenecyclohexyl)methyl radical 3 at 25 deg C is 4.4 x 102 s-1, which is considerably slower than that (2.3 x 105 s-1) of the parent 5-hexenyl radical.The energy of activation for the process 3 -> 4 is 12.8 kcal mol-1, which is in excellent agreement with theoretical values derived from force-field calculations.Ring-closure of appropriately substituted (4-methylenecyclohexyl)methyl radical precursors allows the synthesis of bicycloheptyl systems with useful functionality at the bridgehead to be achieved readily and in high yield.An interesting example is given of the application of an iodine-atom-transfer cyclization to the synthesis of a bicycloheptane functionalized at C7 and C1.
- Della, Ernest W.,Knill, Andrew M.,Pigou, Paul E.
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p. 2110 - 2114
(2007/10/02)
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- SUBSTITUTED TETRAHYDROBENZOTHIAZOLES AS DOPAMINERGIC AGENTS
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Substituted tetrahydrobenzothiazoles are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful as dopamine agonists with selectivity for the presynaptic dopamine receptor and are useful as dopaminergic, antipsychotic, and antihypertensive agents as well as for treating hyperprolactinaemia-related conditions and central nervous system disorders.
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- Dialkyl-substituted dithianes and pesticidal compositions
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The present invention provides compounds of the formula (I): STR1 wherein m and n are independently selected from 0, 1 or 2, STR2 R is selected from hydrogen, methyl or ethyl; R1 is selected from C1-4 hydrocarbyl substituted by one to five halo atoms, and a group --C C--R9 wherein R9 is a group S(O)w --R10 wherein R10 is trifluoromethyl, methyl or ethyl and w is 0, 1 or 2 or R9 is a C3-5 aliphatic group or an aliphatic group containing up to 5 carbon atoms atoms substituted by C1-4 alkoxy, C2-6 alkoxyalkoxy, C1-8 acyloxy, halo or hydroxy, a group COR11 wherein R11 is hydrogen, C1-4 alkyl, C1-4 alkoxy or a group NR12 R13 wherein R12 and R13 are independently selected from hydrogen, methyl or ethyl, or R9 is SiR14 R15 R16 wherein R14 to R16 are the same or different and each is a C1-4 aliphatic group or R14 and R15 are C1-4 aliphatic groups and R16 is a phenyl group; R2, R3, R7 and R8 are independently selected from hydrogen, methyl or halo; R4a and R4b, R6a and R6b are independently selected from hydrogen, C1-3 alkyl, C2-3 alkenyl or alkynyl each being optionally substituted by halo, cyano or C1-4 alkoxy; cyano, halo or a group COR 11a wherein R11a is hydrogen, C1-4 alkoxy, C1-4 alkyl or a group NR12a R13a wherein R12a and R13a are independently selected from hydrogen, methyl or ethyl; R5a is a non-aromatic hydrocarbyl group containing up to seven carbon atoms, or phenyl each optionally substituted by cyano, halo, C1-4 alkyl, C1-4 haloalkyl, C3-4 cycloalkyl, C1-4 alkoxy or a group S(O)q R17 wherein q is 0, 1 or 2 and R17 is methyl or ethyl and R5b is hydrogen, hydroxy or C1-4 alkyl optionally substituted by alkoxy; and represents --CH--CH-- or --C=C-- which are useful pesticides, processes for their preparation, pesticidal formulations containing them and their use in the control or prevention of pest infestation.
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- 4,4-bis(4-hydroxyphenyl)cyclohexanecarboxylic acid derivatives and process for preparing same
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Novel 4,4-bis(4-hydroxyphenyl)cyclohexanecarboxylic acid derivatives. These compounds can be prepared by reacting a cyclohexanone-4-carboxylic acid with a phenol.
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- Process for preparing alkyl substituted para-carboalkoxy cyclohexanones
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Described are para-carboalkoxy cyclohexanones defined according to the structure: STR1 wherein R1 represents hydrogen or C1 -C7 alkyl and R2 represents methyl or ethyl and uses thereof in augmenting or enhancing the aroma of consumable materials including foodstuffs, chewing gums, toothpastes, medicinal products, chewing tobaccos, perfume compositions, colognes and perfumed articles (e.g., solid or liquid anionic, cationic, nonionic or zwitterionic detergents, cosmetic compositions, fabric softener compositions, fabric softener articles, hair preparations and perfumed polymers. The compounds defined according to the structure: STR2 wherein R1 ' represents C4 -C7 alkyl and R2 represents methyl or ethyl are novel compounds.
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- FACILE SYNTHESIS OF 4-CARBETHOXYCYCLOHEXANONE
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A facile decarboalkoxylative route to 4-carbethoxycyclohexanone (1) from the tricarbethoxy derivative 3 is described.
- Sanchez, Ignacio H.,Ortega, Armando,Garcia, Gabriel,Larraza, Maria Isabel,Flores, Humberto J.
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p. 141 - 150
(2007/10/02)
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- FURTHER EXTENSIONS OF THE KINETIC ENOLATE METHOD FOR TERPENOID SYNTHESES
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New stereorandom syntheses of juvabione and dehydrojuvabione using kinetic enolates as synthons are described.
- Ferrino, S. A.,Maldonado, L. A.
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p. 925 - 932
(2007/10/02)
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- Synthesis of aminoiderivatives of 4,5,6,7-tetrahydro-benzothiazole. II. 4, 5 and 6-aminomethyl derivatives with cardiovascular activity
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The ethyl esters of 4,5,6,7-tetrahdyro-benzothiazolyl-4 carboxylic acids were synthesized from corresponding ethyl 1-oxo-2 bromo-cyclohexane-carboxylates. Their reduction to alcohols, which were then transformed into tosylates, leads to the aminomethyl derivatives. These derivatives are practically devoid of antihistaminic H2 and dopaminergic activities but have interesting cardiovascular properties.
- Maillard,Delaunay,Langlois,et al.
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p. 457 - 460
(2007/10/02)
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- Synthetic Studies in Carbocyclic Systems : Part I - A new Synthesis of Nopinone
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Base-induced intramolecular nucleophilic displacement of the tosyloxy group of 4-isopropyl-7-tosyloxycyclohexanone affords nopinone , identical with an authentic specimen.
- Murthi, G. S. S.,Mazumder, Alok
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p. 339 - 340
(2007/10/02)
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