Abstract: In producing optically-active amino acid benzyl esters by reacting optically-active amino acids with benzyl alcohols, hydrazines are present in the reaction system, or the compounds are reacted in the absence of oxygen, or the compounds are reacted in the absence of oxygen while hydrazines are present in the reaction system. The processes are simple and give optically-active amino acid benzyl esters of high optical purity.
Abstract: Novel acetyloxymethyl esters are disclosed. Methods of treating an illness, including cancer, hemological disorders and inherited metabolic disorders, and treating or ameliorating other conditions using these compounds are also disclosed. The compounds are effective in the inhibition of histone deacetylase.
Type:
Grant
Filed:
January 28, 2002
Date of Patent:
March 2, 2004
Assignee:
Beacon Laboratories, Inc.
Inventors:
Hsuan-Yin Lan-Hargest, Norbert L. Wiech
Abstract: The present invention provides non-hygroscopic, crystalline salts of levodopa ethyl ester (LDEE), wherein the salt is the octanoate salt, the myristate salt, the succinate salt, the succinate dihydrate salt, the fumarate salt or the fumarate dihydrate salt of levodopa ethyl ester. The subject invention also encompasses compositions comprising a levodopa ethyl ester salt and a carrier and processes for making these compositions. In addition, the subject invention concerns pharmaceutical compositions comprising a levodopa ethyl ester salt and a pharmaceutically acceptable carrier, as well as processes for making these pharmaceutical compositions.
Abstract: There is provided a method for obtaining an alkyladamantyl ester efficiently by distilling and purifying a crude alkyladamantyl ester containing impurities which decompose the alkyladamantyl ester without decomposing the alkyladamantyl ester.
The crude alkyladamantyl ester such as crude 2-methyl-2-adamantyl methacrylate is distilled in the presence of a heterocyclic compound and/or a basic compound such as 3-ethyl-3-hydroxymethyloxetane or diglycidyl bisphenol A.
Abstract: 3-(3-Methyl-4-hydroxyphenyl)-3-methylbutyl aldehyde may be produced from 3-(3-methyl-4-hydroxyphenyl)-3-methylbutyric acid by converting the carboxyl group into a formyl group. N-[N-[3-(3-methyl-4-hydroxyphenyl)-3-methylbutyl]-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester, which is useful as a sweetener having a high potency of sweetness, can be easily and efficiently prepared on an industrial production from such an aldehyde derivative, via a reductive alkylation reaction with aspartame. Therefore, 3-(3-Methyl-4-hydroxyphenyl)-3-methylbutyl aldehyde is extremely excellent as an intermediate for the production of N-[N-[3-(3-methyl-4-hydroxyphenyl)-3-methylbutyl]-L-&agr;-aspartyl]-L-phenylalanine 1-methyl ester.
Abstract: Fluorinated multifunctional alcohols containing at least 3 primary hydroxyl groups are disclosed. Such alcohols allow for easy synthesis of multifunctional crosslinkers such as acrylates, epoxies and vinyl ethers. The multifunctional crosslinkers are used in fluorinated optical coating and waveguide compositions to increase curing speed and crosslinking density.
Type:
Grant
Filed:
January 31, 2002
Date of Patent:
February 10, 2004
Assignees:
E. I. du Pont de Nemours and Company, Telephotonics Incorporated
Inventors:
Fang Wang, Baopei Xu, Indira S. Pottebaum, Chuck C. Xu
Abstract: The present invention is a novel intermediate, compound of the formula (VI)
and salts thereof. In addition, the invention includes a process for the preparation of a 15(S)-prostaglandin intermediates compounds (IV) and (XVIII) which comprises (1) contacting a the corresponding enone with (−)-chlorodiisopinocampheylborane while maintaining the reaction mixture temperature in the range of from about −50° to about 0° and (2) contacting the reaction mixture of step (1) with a boron complexing agent.
Abstract: The present invention relates to the field of organic synthesis and more specifically to a process for the preparation of Michael-adducts, as defined below, by reacting a &bgr;,&bgr;- or a &agr;,&bgr;-disubstituted, or a &agr;,&bgr;,&bgr;-trisubstituted, &agr;,&bgr;-unsaturated ketone (I) with a &bgr;-ketoester or a &bgr;-diketone (II) in presence of a suitable catalyst of formula M(X)n, according to scheme 1:
Abstract: The present invention relates to a new and industrially advantageous process for the preparation of 3-ethoxy-4-ethoxy-carbonyl-phenyl acetic acid. This compound is a key intermediate for the synthesis of Repaglinide, an oral hypoglycemic agent.
Type:
Grant
Filed:
September 20, 2002
Date of Patent:
February 3, 2004
Assignee:
Banbaxy Laboratories Limited
Inventors:
Mohammad Salman, J. Suresh Babu, Purna C. Ray, Sujay Biswas, Naresh Kumar
Abstract: A process for the production of acetic acid by reacting carbon monoxide with methanol and/or a reactive derivative thereof in a liquid reaction composition comprising an iridium carbonylation catalyst, methyl iodide, methyl acetate, water and acetic acid characterised in that there is also present in the reaction composition a monodentate phosphine oxide compound in an amount of up to and including 200 mol per gram atom of iridium.
Abstract: Compounds of formula (I), wherein R1 and R2 are, independently of one another, H, C1-C6alkyl, C1-C6halogenalkyl, C1-C6alkoxy, C1-C6alkoxy-C1-C6alkyl, or C1-C6alkoxy-C1l-C6alkyloxy, and R3 is C1-C6alkyl, are obtainable in high yields by stereoselective addition of R3-substituted propionic acid esters to R1- and R2-substituted benzaldehydes of formula R—CHO to form corresponding 3-R-3-hydroxy-2-R3-propionic acid esters, conversion of the OH group to a leavaing group, subsequent regioselective elimination to form 3-R-2-R3-propenic acid esters, and their hydrolysis to form corresponding propenic carboxylic acids and their enantioselective hydrogenation, wherein R is (a).
Type:
Grant
Filed:
January 2, 2003
Date of Patent:
January 27, 2004
Assignee:
Speedel Pharma AG
Inventors:
Stefan Stutz, Peter Herold, Felix Spindler, Walter Weissensteiner, Thomas Sturm
Abstract: A polyether-polyol compound represented by the compositional formula C3nH6n+2O2n+1, wherein n is an integer of 4 or more, wherein the polyether-polyol compound has a total number of 1,2-diol unit and 1,3-diol unit of [(n/2)+1] in a case where n is an even number of 4 or more, or a total number of 1,2-diol unit and 1,3-diol unit of [((n−1)/2)+1] and one hydroxyl group which is not involved in the units in a case where n is an odd number of 5 or more; a polyglycerol alkyl ether, a part of hydroxyl groups in a polyglycerol being substituted by an alkyl group, wherein the polyglycerol is the polyether polyol compound mentioned above; and an ester prepared by the process comprising reacting the polyether-polyol compound mentioned above or the polyglycerol alkyl ether mentioned above with a fatty acid.
Abstract: The present invention relates to a production method of (R)-3-hydroxy-3-(2-phenylethyl)hexanoic acid which comprises optical resolution of racemic 3-hydroxy-3-(2-phenylethyl)hexanoic acid with an optically active amine of the formula (VIII)
wherein R2 is 3,4-dimethoxyphenyl or 2-chlorophenyl. According to the present invention, (R)-3-hydroxy-3-(2-phenylethyl)hexanoic acid useful as a starting material of a pharmaceutical agent can be efficiently produced with a high optical purity and a relatively high total yield.
Abstract: Alcohol alkoxylates of the formula (I)
R1—O—(CH2—CHR5—O—)r(CH2—CH2—O—)n(CH2—CHR6—O—)s(CH2—CHR2—O—)mH (I)
where
R1 is an at least singly branched C4-22-alkyl
R2 is C3-4-alkyl
R5 is C1-4-alkyl
R6 is methyl or ethyl
n is an average value from 1 to 50
m is an average value from 0 to 20
r is an average value from 0 to 50
s is an average value from 0 to 50,
where m is at least 0.5 if R5 is methyl or ethyl or r is 0, or alcohol alkoxylates of the formula (II)
R3—O—(CH2—CH2—O—)p(CH2—CHR4—O—)qH (II)
where
R3 is branched or unbranched C4-22-alkyl
R4 is C3-4-alkyl
p is an average value of from 1 to 50
q is an average value of from 0.5 to 20
are used as low-foam or foam-suppressing surfactants.
Type:
Grant
Filed:
October 7, 2002
Date of Patent:
January 20, 2004
Assignee:
BASF Aktiengesellschaft
Inventors:
Helmut Gümbel, Martin aus dem Kahmen, Norbert Wagner, Klaus Taeger
Abstract: A process for monitoring and controlling reactor conditions during the production of acetic acid by the catalyzed carbonylation of methanol is provided. The process of the present invention comprises measuring the density of the heavy phase of the light ends distillation column in the purification system of the carbonylation process. The density measurement is used to adjust the feed of methanol and/or to regulate the temperature in the reaction zone to optimize reactor conditions. The density measurement may also be used to adjust other parameters in the reactor system. The invention is also directed to the system for manufacturing acetic acid based on the process control procedure described.
Type:
Grant
Filed:
January 28, 2002
Date of Patent:
January 13, 2004
Assignee:
Celanese International Corporation
Inventors:
Michael E. Huckman, G. Paull Torrence, Hung-Cheun Cheung
Abstract: A compound of formula (I)
wherein:
R isopropyl;
n is 0;
R1 is naphthylmethyl;
R2 is t-butyl; and
R3 is methyl;
is useful in the treatment of disorders mediated by s-CD23.
Abstract: Aspirin triggered lipid mediators (ATLMs) are disclosed which are useful for the treatment of prevention of inflammation associated with various diseases, including ischemia.
Abstract: Adamantane derivatives in which two (meth)acryloyloxyalkyl groups are bonded with an adamantane ring through ester groups, adamantane derivatives in which two adamantane rings are bonded through an alkylene group and two urethane bonds, which two adamantane rings each have a (meth)acryloyloxy group bonded thereto directly or through a coupling group, and adamantane derivatives each having a structure in which a group containing an adamantane ring hangs on the alkylene group of an alkylene glycol di(meth)acrylate. The compounds are useful as dental materials intermediates therefor, and as intermediates for optical materials such as lenses.
Abstract: An ester compound of the following formula (1) is provided.
R1 is H, methyl or CH2CO2R3, R2 is H, methyl or CO2R3, R3 is C1-C15 alkyl, R4 is branched or cyclic, tertiary C5-C20 alkyl group, Z is a divalent C1-C10 hydrocarbon group, and k is 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, and etching resistance, and is suited for micropatterning using electron beams or deep-UV.
Type:
Grant
Filed:
November 6, 2002
Date of Patent:
December 30, 2003
Assignee:
Shin-Etsu Chemical Co., Ltd.
Inventors:
Tsunehiro Nishi, Koji Hasegawa, Takeru Watanabe, Takeshi Kinsho, Mutsuo Nakashima, Seiichiro Tachibana, Jun Hatakeyama
Abstract: Provided herein are novel and useful combretastatin A-4 prodrug salts that increase the solubility of combretastatin A-4, readily regenerate combretastatin A-4 in vivo under normal physiological conditions, and which produce physiologically tolerable products as a result of the regeneration of combretastatin A-4.
Type:
Grant
Filed:
September 11, 2001
Date of Patent:
December 30, 2003
Assignee:
Bristol-Myers Squibb Company
Inventors:
John J. Venit, Mandar V. Dali, Manisha M. Dali, Yande Huang, Charles E. Dahlheim, Ravindra W. Tejwani