|7432391||Process for the production of tert-butyl N-(2-bromoethyl)carbamate|
The present invention is to provide a safe process for the production of tert-butyl N-(2-bromoethyl)carbamate where operation is simple, handling of the final product is easy, working efficiency is good and yield is high. A process for the production of tert-...
The invention relates to novel triazolopyrimidines of the formula in which R1, R2, R3 and X have the meanings given in the disclosure, and acid addition s...
|6794384||Hydroxylation activated drug release|
The present invention concerns prodrugs whose aromatic oxidation, particularly their enzymatic aromatic hydroxylation, results in their activation by the release of a drug moiety. It particularly concerns anti-tumor prodrugs and those which are specifically activate...
|6639094||Process for producing -aminoketone derivatives|
A process for producing -amino-dihalogenated methyl ketone derivatives by reacting an N-protected -amino acid ester with a dihalomethyl lithium is provided. This process is suitable for the production on an industrial scale and by this proce...
|6399628||N-(aryl/heteroaryl) amino acid esters, pharmaceutical compositions comprising same, and methods for inhibiting alpha- amyloid peptide release and/or its synthesis by use of such compounds|
Disclosed are compounds which inhibit ଲ-amyloid peptide release and/or its synthesis, and, accordingly, have utility in treating Alzheimer's disease. Also disclosed are pharmaceutical compositions comprising a compound which inhibits ଲ-amyloid...
|6204361||Method of peptide synthesis|
The present invention relates to a process for forming an N--amino protected amino acid fluoride in situ by reacting an N--amino protected amino acid with an ionic fluoride salt in the presence of a peptide coupling agent. It is also directe...
|6160161||Per(poly)fluorinated polyoxyethylated carbamates|
Per(poly)fluorinated polyoxyethylated carbamates of general formula (I) in which RF represents a perfluorinated group containing between 1 and 18 carbon atoms, W represents an oxo group or nothing, n is an integer from 1 to 10, m is from values...
|6040422||Synthesis and use of amino acid fluorides as peptide coupling reagent|
The present invention is directed to a process for forming a peptide bond between a first amino acid having a free amino group and a protected carboxy group and a second amino acid or between a peptide having a free amino group and a blocking carboxy grou...
|6020518||Process for preparing ଲ-amino--hydroxy acid derivatives|
An object of the present invention is to provide a process for producing a ଲ-amino--hydroxy acid derivative via efficient and industrially utilizable steps. The present invention provides a process for producing a ଲ-amino--hydrox...
|5750767||Synthesis and use of amino acid fluorides as peptide coupling reagents|
The present invention is directed to the process of preparing a peptide comprising reacting a first amino acid or peptide with an amino acid fluoride of the formula: ##STR1## or the acid fluoride salts thereof wherein BLK is an N-amino protecting ...
|5688795||3-(4-phenylpiperazin-1-yl)propyl-amino, thio and oxy!-pyridine, pyrimidine and benzene derivatives as 1 -adrenoceptor antagonists|
The present invention relates to novel 댑 -adrenoceptor antagonists of Formula I: ##STR1## in which: p is 0 or 1; t is 0, 1 or 2; X is O, S or NR6 (in which R6 is hydro or (C1-6)alkyl); Y and Z are indepen...
|5643438||Process for the preparation of substituted diamino-dicarboxylic acid derivatives|
The invention relates to a new process for the preparation of substituted diaminodicarboxylic acid derivatives of the formula ##STR1## in a high yield by a modified Kolbe synthesis....
|5523463||Method of producing halogenated and alpha-aminoalchohols|
A process for the manufacture of N-protected -aminoketones and N-protected -aminoalcohols of the formula ##STR1## wherein X is halogen, one of Q1 and Q2 is hydrogen and the other is hydroxy or Q1 and Q
|5502225||Perfluoroalkyl terminated urethane lubricants|
This invention relates to perfluoroalkyl group terminated urethanes, thiourethanes and ureas of the general formula (R--X--CONH)m A where m is 1, 2 or 3, R is Rf -E and optionally R1 with the proviso that at least one R is R
|5476974||Omega-hydrofluoroalkyl ethers, precursor carboxylic acids and derivatives thereof, and their preparation and application|
Normally liquid, omega-hydrofluoroalkyl ether compounds (and selected mixtures thereof) have a saturated perfluoroaliphatic chain of carbon atoms interrupted by one or more ether oxygen atoms. The compounds can be prepared, e.g., by decarboxylation of the...
|5442088||Process for the preparation of phosphorus-containing L-amino acids, their derivatives and intermediates for this process|
Process for the preparation of phosphorus-containing L-amino acids, their derivatives and intermediates for this process L-amino acids of the formula I and salts thereof, ##STR1## in which R1 to R5 are defined as in claim 1 and n is ...
|5360928||Synthesis and use of amino acid fluorides as peptide coupling reagents|
A compound of the formula ##STR1## or the acid fluoride salts thereof wherein BLK is an N-amino protecting group or hydrogen AA is an amino acid residue and X is H or a protecting group useful as a coupling agent in peptide synthesis....
|5198569||Process for the preparation of optically active aliphatic hydroxycarboxylic acids|
The asymmetric hydrogenation of aliphatic -keto esters in the presence of rhodium catalysts which contain as chiral ligand a diphosphine of formula IV (R3)2 P--Q--P(R3)hd 2 (IV) wherein R3
|5194660||Processes for producing carbamates and isocyanates|
Processes for producing carbamates comprise contacting a first reactant selected from primary amine components, secondary amine components, urea components and mixtures thereof; carbon monoxide; at least one organic hydroxyl component and at least one oxy...
|5102911||4-Substituted HMG-CoA reductase inhibitors|
HMG-CoA reductase inhibitors of formulae (I) and (II) are disclosed. ##STR1##...
|5078783||Substituted alkyl carbamates and their use as herbicides|
Substituted 1-alkyl carbamates of the formula ##STR1## in which: R is a member selected from the group consisting of halogen, trifluoromethyl, cyano, NO2 and C1 -C3 haloalkyloxy; R1 is selected from the group co...
|5037991||Novel substituted aromatic compounds|
Substituted phenoxy, phenylthio and anilino compounds, intermediates therefor, synthesis thereof, and their use for the control of pests....
|5017718||Process for preparing polyfluoroalkyl-substituted compounds|
A process for preparing a perfluoroalkyl-substituted compound is disclosed. The process comprises reacting a halopolyfluoroalkane having 1 to 20 carbon atoms with a compound selected from the group consisting of (1) a substituted or unsubstituted ethylene...
|5001148||Mevinic acid derivatives|
Antihypercholesterolemic activity, due to competitive inhibition of HMG CoA reductase, has been found in compounds of the formula ##STR1## wherein: R1, R2 and R3 are independently selected from: (1) alkyl, (2) substituted ...
|4987248||Acid catalyzed formation of carbamates from olefins|
An improved for preparing N-substituted carbamate comprising reaction of a selected olefin or alcohol with a carbamate in the presence of a catalyst comprising a blend of a perfluorinated sulfonic acid polymer and a perfluorinated polymer diluent in a sub...
Alkyl esters of 2-fluoro-1-methoxyethylcarbamic acid, which are useful intermediates in the preparation of compounds, such as 4-amino-5- fluoropentanoic acid, are prepared by the electrochemical anodic oxidation of esters of 2-fluoroethylcarbamic acid in ...
|4786745||2,2-dihalovinyl haloformates and process of preparation|
Novel 2,2-dihalovinyl haloformates are described of general formula: ##STR1## in which: X is a chlorine or bromine atom; X1 and X2 are the same or different and are chlorine or bromine. The compounds are prepared by reaction of a 1,2,2,2-...
|4772695||Process for the preparation of vinyl carbamates|
A process for the preparation of vinyl carbamates of formula I ##STR1## is described which comprises heating an -halogeno-carbamate of formula II ##STR2## in which X is a halogen atom at a temperature between 70° and 250° C. for a ...
|4760057||(Acyloxyalkoxy)carbonyl derivatives as bioreversible prodrug moieties for primary and secondary amine functions in drugs|
This invention relates to novel (acyloxyalkoxy)carbonyl derivatives as bioreversible prodrug moieties for primary and secondary amine functions in drugs having a primary or secondary amine function thereon. Hydrolytic enzymes are used to trigger the regen...
|4740600||Photolabile blocked surfactants and compositions containing the same|
Surfactants which are blocked against surfactant action (identified herein as "photolabile blocked surfactants") by a photolabile protective or masking group but which, on exposure to actinic radiation, become unblocked are provided. Coating compositions ...
|4697033||Carbamic and carbamothioic acid esters as pesticides|
Certain novel derivatives of carbamates and their use for the control of pests....
This invention is for γ-allenyl-γ-aminobutyric acid derivatives which are γ-aminobutyric acid transaminase inhibitors....
|4609648||Halogenoalkylcarbamic acid ester pesticides|
Halogenoalkylcarbamic acid esters of the formula ##STR1## in which R, R1 and R2 independently of one another represent methyl which is optionally substituted by halogen, at least one of the methyl groups R, R1 and R
|4603216||Process for the preparation of urethanes|
This invention relates to a process for preparing urethanes by reacting a solution of a nitrogen-containing organic compound and a hydroxyl-containing organic compound with carbon monoxide in the presence of a ruthenium catalyst comprising a bis phosphine...
|4594441||Process for the preparation of urethanes|
A process for the preparation of urethanes. Urethanes having the general formula R1 (NHCOOR2)n are reacted with an alcohol at a temperature of 120° to 400° C. in amounts such that, for every mol of the urethane, at least...
|4554372||Preparation of carbamates|
2-Substituted alkyl (2-substituted alkyl)carbamates useful as intermediates in the preparation of epoxy derivatives of olefins are prepared by reacting 2-oxazolidones with an olefin and an electrophile such as halogen....
|4549994||Preparation of new fluoropivalic acid fluorides|
A process for the preparation of a compound according to claim 1, comprising reacting a compound of the formula ##STR1## in which R3, R4 and R5 each independently is CH3 or CH2 Cl, at least one o...
|4511730||Carbamates of beta-hydroxyethylsulfoxides|
This invention relates to carbamates of beta-hydroxyethylsulfoxides which are useful as cosurfactants in enhanced oil recovery, surfactants and biocides, and as hydraulic fluids when of sufficiently low molecular weight....
|4505859||Preparation of 2-haloethylamides|
2-Haloethylamides are prepared by reaction of 2-oxazolidinone or C1-6 alkyl or phenyl derivatives thereof with an acid halide....
|4448773||Microbicidal N-alkoxycarbonyl-alkyl-N-substituted acetyl-anilines and -naphthylamines|
Compounds of the formula ##STR1## in which Ar is 2-alkyl-, -alkoxy- or -halo-methyl-phenyl or -naphthyl, each of which is further substituted, R1 is 2-furyl, 2-tetrahydrofuryl, alkenyl, cyclopropyl, ଲ-alkoxyethyl, hydroxymethy...