Abstract: The present invention relates to an integrated process for the preparation in continuous of epoxides which comprises: (a) preparing an alcoholic or hydro-alcoholic solution of hydrogen peroxide in a concentration of over 3% by weight, using a gaseous stream containing hydrogen, oxygen and an inert gas, in the presence of a bimetallic catalyst based on palladium and platinum as active components; (b) putting the alcoholic or hydro-alcoholic solution of hydrogen peroxide obtained in step (a) in contact with an olefin and a buffering agent, in the presence of an epoxidation catalyst suspended in the reaction solvent, in order to obtain a reaction mixture containing the epoxide corresponding to the olefin, water and the alcoholic solvent; (c) treating the alcoholic stream leaving step (b), after separation of the epoxide, in order to eliminate the nitrogenated compounds present; (d) feeding the alcoholic solvent obtained in (c) to step (a).
Type:
Grant
Filed:
June 26, 2002
Date of Patent:
April 1, 2003
Assignee:
Polimeri Europa S.r.l.
Inventors:
Giuseppe Paparatto, Anna Forlin, Giordano De Alberti, Rino D'Aloisio, Paolo Tegon
Abstract: Taxane prodrugs comprise a taxane joined by a hydrolyzable bond to one or more oligomers that comprise a polyethylene glycol moiety. The oligomer preferably further comprises a salt-forming moiety.
Type:
Grant
Filed:
March 9, 2001
Date of Patent:
April 1, 2003
Assignee:
Nobex Corporation
Inventors:
Nnochiri N. Ekwuribe, Christopher H. Price, Gary S. Bartley
Abstract: Disclosed is a method for producing compounds of formula (I), wherein R1 represents H or (CH2)mOH, R2 represents H or (CH2)nOH, R3 represents H or (CH2)pOH and m, n and p represent 2-8 independently from one another. Said compounds are particularly suitable for use as food supplements. They are highly suitable for use in cosmetic formulations as UV filters, for instance.
Type:
Grant
Filed:
April 25, 2001
Date of Patent:
March 25, 2003
Assignee:
Merck Patent Gesellschaft
Inventors:
Herwig Buchholz, Ralf Rosskopf, Alice Lichtenberg, Christine Kraus
Abstract: The present invention provides a novel semi-synthetic method of producing a variety of novel taxane derivatives. The method involves the reaction of a phenylisoserine derivative with a suitably blocked Baccatin III derivative to produce a taxane substrate that may be further modified to form Pactitaxel and other potentially useful taxane derivatives.
Type:
Grant
Filed:
March 23, 2001
Date of Patent:
March 11, 2003
Assignee:
Scinopharm Taiwan, Ltd.
Inventors:
George Schloemer, Yung-Fa Chen, Chien Hsin Lin, Wlodzimierz Daniewski
Abstract: Enantiomerically enriched hydroxychromanones are obtained by the AlCl3-catalyzed intramolecular Friedel-Crafts acylation of the corresponding 3-phenoxy-2-alkylcarbonyloxy-propionic acid followed by cleavage of the carboxylate in the presence of an alkali metal peroxide or hydroperoxide. Enantiomerically enriched cis-aminochromanols can then be prepared by treating the hydroxychromanones with a hydroxylamine and hydrogenating the resulting oxime. The cis-aminochromanols can be employed as intermediates in the production of HIV protease inhibitors which are useful for treating HIV infection and AIDS.
Type:
Grant
Filed:
October 24, 2001
Date of Patent:
March 11, 2003
Assignee:
Merck & Co., Inc.
Inventors:
Karl Hansen, Paul Devine, Philippe M. Rabbat
Abstract: Epoxyalkanes are subjected to at least one of the following washing operations: (1) washing with aqueous inorganic base, and then with aqueous borohydride, or vice versa; or (2) washing with an aqueous solution of both inorganic base and borohydride. Undesirable odor is reduced or eliminated from alkanediol(s), if produced from the treated epoxyalkane(s) by hydrolysis. Use of such washing procedures in the production of alkanediols is also described.
Type:
Grant
Filed:
April 3, 2002
Date of Patent:
March 4, 2003
Assignee:
Albemarle Corporation
Inventors:
Chi Hung Cheng, Gerald M. Sulzer, John F. Balhoff
Abstract: This invention provides a process for producing an epoxy compound industrially advantageously at low cost in a short process. Furthermore, this invention provides a novel fruity, camphoric, floral, amber or woody fragrance-, flavor- or scent-imparting composition containing said epoxy compound, and foods & drinks, perfumes, cosmetics and tobaccos containing said composition.
The epoxy compound can be produced by letting an &agr;-halocyclododecanone and an organic magnesium compound react with each other for Grignard reaction, hydrolyzing to obtain a halohydrin and letting the halohydrin and a base react with each other in the presence of an phase transfer catalyst or adding an aprotic polar solvent for reaction.
Abstract: Mixed together are (i) hydrogen peroxide; (ii) 1-alkene; (iii) quaternary ammonium salt wherein at least one of the substituents contains at least six carbon atoms; (iv) boric acid, or both a 1,2-diol and boric acid; and (v) a preformed catalyst solution formed from hydrogen peroxide, at least one aqueous inorganic acid, and at least one tungstate salt, while water is continuously removed, such that a 1,2-epoxide is formed. A new method for purifying 1,2-epoxyalkanes is also described.
Abstract: The invention relates to a process for the preparation of Fumagillin by liberation from its salt characterized by reacting Fumagillin dicyclohexylamine salt with an organic acid in alcoholic medium.
Type:
Grant
Filed:
March 5, 2002
Date of Patent:
February 18, 2003
Assignee:
Sanofi-Synthelabo
Inventors:
Gyula Farkas, Andrea Györbiró, István Hermecz, Kálmán Simon, Anna Szabó, Árpádné Vasvári
Abstract: The novel compositions and methods of the subject invention can be used in antifugal applications. The antifugal agents of the subject invention can be used in the treatment of an animal or human having a fugal infection. In a further embodiment the compounds can be used to treat plant fugal infections, disinfect surfaces, and prevent spoilage of organic compositions such as food and cosmetics.
Type:
Grant
Filed:
July 20, 2001
Date of Patent:
February 18, 2003
Assignees:
Harbor Branch Oceanographic Institution, Inc., Mycologics, Inc.
Inventors:
Ying Chen, Katherine Chilson, Keith Brian Killday, Dedra Harmody, Peter J. McCarthy, Shirley A. Pomponi, Rebecca Schimoler, Claude Selitrennikoff, Amy E. Wright
Abstract: Disclosed is a process for the preparation of 3-methyltetrahydrofuran (MeTHF) from 3-(hydroxymethyl)tetrahydrofuran (HOMeTHF) by contacting HOMeTHF with hydrogen in the presence of an acidic, supported catalyst comprising a Group VIII metal.
Type:
Grant
Filed:
April 18, 2002
Date of Patent:
February 18, 2003
Assignee:
Eastman Chemical Company
Inventors:
Alexey Victorovitch Ignatchenko, William Anthony Beavers, Zhufang Liu
Abstract: Cyclic acetal compounds of formula (1) wherein k=0 or 1 and n is an integer of 0 to 6 are novel. Using the cyclic acetal compounds as a monomer, polymers are obtained. A resist composition comprising the polymer as a base resin is sensitive to high-energy radiation and has excellent sensitivity, resolution, and etching resistance.
Type:
Grant
Filed:
October 2, 2001
Date of Patent:
February 4, 2003
Assignee:
Shin-Etsu Chemical Co., Ltd.
Inventors:
Mutsuo Nakashima, Seiichiro Tachibana, Takeru Watanabe, Takeshi Kinsho, Koji Hasegawa, Tsunehiro Nishi, Jun Hatakeyama
Abstract: A process for production of an oxetane, which process comprises subjecting an alcohol having two or more hydroxyl groups to reaction with a carbamide at a molar ratio employing 1-2 moles of said carbamide on 1-2 moles of said alcohol. The alcohols preferably have at least one 1,3-diol grouping. The reaction is carried out in the presence of at least one catalyst promoting and/or initiating transcarbonylation and/or pyrolysis. A reaction mixture comprising an oxetane and optionally an orthocarbonate of said alcohol is yielded. The oxetane is suitable recovered from said reaction mixture by for instance distillation.
Abstract: Insoluble resinous sodium materials are separated from a hydroperoxide/olefin epoxidation feed by contact with a fine screen or a bed of coalescing solids.
Abstract: A process is provided for use in the conversion of alkanes into alkylene oxides, having particular utility in the conversion of propane to form propylene oxide, using a lanthanide-promoted, supported, silver catalyst prepared via precipitation. A preferred embodiment uses silver nitrate and lanthanum nitrate to form the catalyst on a BaCO3 support.
Type:
Grant
Filed:
February 22, 2001
Date of Patent:
January 21, 2003
Assignee:
SRI International
Inventors:
Guido Mul, Marianna F. Asaro, Albert S. Hirschon, Robert B. Wilson, Jr.
Abstract: The present invention relates to chemical compounds that are useful in the production of taxanes. The chemical compounds according to the present invention have a generalized formula:
wherein R1 is +NH3X− where X is deprotonated organic acid such as deprotonated trifluoroacetic acid, and wherein R2 may be acetyl or hydrogen, and P1 may be hydrogen or a hydroxyl protecting group, such as benzyloxymethyl.
Abstract: The present invention provides an alkoxylation solid catalyst with which an alkylene oxide adduct having a narrow adduct distribution can be produced while inhibiting formation of high molecular weight polyalkylene glycol having a molecular weight of about tens of thousands as a by-product. The alkoxylation catalyst comprises a metal oxide containing magnesium, aluminum, and at least one metal selected from the metals that belong to group VIA, group VIIA, and group VIII as a third component. The third component metal changes the structure of the active site in the catalyst, for example, by forming a metal oxide having a spinel-type structure with aluminum (e.g. when the third component metal is Mn, MnAl2O4 is formed), so that a side reaction of forming a high molecular weight polyalkylene glycol is inhibited.
Abstract: An ester compound of formula (1) is provided.
R1 is H or methyl, R2 is tertiary C4-20 alkyl, and k=0 or 1. A resist composition comprising as the base resin a polymer resulting from the ester compound is sensitive to high-energy radiation, has excellent sensitivity, resolution, etching resistance and substrate adhesion, and is suited for micropatterning using electron beams or deep-UV.
Type:
Grant
Filed:
June 5, 2001
Date of Patent:
December 31, 2002
Assignee:
Shin-Etsu Chemical Co., Ltd.
Inventors:
Takeru Watanabe, Takeshi Kinsho, Koji Hasegawa, Tsunehiro Nishi, Mutsuo Nakashima, Seiichiro Tachibana, Jun Hatakeyama
Abstract: A process for producing oxidized organic chemical products such as propylene oxide from various organic chemical feedstocks utilizing as oxidant directly produced hydrogen peroxide (H2O2) intermediate oxidizing agent. The hydrogen peroxide intermediate is directly produced from hydrogen and oxygen feeds plus a suitable solvent in a first catalytic reaction step utilizing an active supported phase-controlled noble metal catalyst at reaction conditions of 0-100° C. temperature and 300-3,000 psig pressure. An organic chemical feedstock such as propylene together with the hydrogen peroxide intermediate and solvent solution are fed into a second catalytic reactor maintained at 0-150° C. temperature and 15-1,500 psig pressure and oxidized to produce a desired crude oxidized organic product such as propylene oxide, which is purified by distillation steps and recovered from the solvent solution.