Abstract: The invention relates to a process allowing the preparation of a (dialkylphosphono)alkyl (meth)acrylate, corresponding to the formula: 1

Abstract: The present invention relates to a new process for the preparation of acetylcholinesterase inhibitors of formula (I) or a salt thereof, wherein: R1 is N-acyl-4-piperidyl; N-alkoxycarbonyl-4-piperidyl; N-alkyl-4-piperidyl; N-benzyl-4-piperidyl; N-(&ohgr;-aralkyl)-4-piperidyl; 4-pyridyl; R4, R5, R6, and R7 are identical or different and each represents hydrogen, straight-chain or branched alkyl, aryl, hydroxy, alkoxy, aryloxy, benzyloxy, acyloxy, alkylthio, arylthio, benzylthio, acylamino, phthalimido or halogen; n is 1, 2 or 3; m is 1, 2, 3, 4, or 5. This process comprises cyclisation of a compound of formula (II) or salts thereof, wherein R1, R4, R5, R6 and R7, m and n are as defined above; R2 is selected from a derivatised or non-derivatised carboxyl, cyano, N-substituted aminocarbonyl groups or hydrogen; R3 is selected from a derivatised or non-derivatised carboxyl, cyano or N-substituted aminocarbonyl groups, optionally in the presence of acids and/or solvents.

Abstract: This invention provides analogues of phosphatidylinositol-phosphates modified at one or more selected inositol-hydroxyls and optionally carrying reporter or anchoring groups attached in the lipid or the inositol residues, and, the synthetic intermediates and methods for the preparation of these analogues. The analogues are useful as research reagents in biomedical studies related to structure, function and therapeuticals, including reference materials for analyzing the metabolic products in safety and efficacy studies of 2- and/or 3-hydroxyl modified inositols and phosphatidylinositols as drug candidates.

Abstract: Glufosinate and the 2-methyl analog thereof can be prepared in a multi-step synthesis from methylphosphorus compounds (II) with unsaturated keto compounds (III) via adducts (IV), subsequent reaction under the conditions of a Strecker synthesis and finally hydrolysis of the aminonitrile (V): Step 1: Step 2: Step 3: Hydrolysis of (V) to give glufosinate Depending on process conditions and substrates, various compounds can be identified as adducts (IV).

Abstract: Compounds of the formula I 1

Abstract: The present invention relates to phosphonic acid derivatives that inhibit N-Acetylated &agr;-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, to treat a glutamate abnormality and to treat a prostate disease in an animal.

Abstract: The present invention relates to a process for the preparation of phosphinic acid esters, which comprises a) reacting elemental yellow phosphorus with alkylating agents in the presence of a base to give a mixture which comprises, as principal constituents, the (metal) salts of alkylphosphonous, phosphorous and hypophosphorous acids, b) esterifying the principal constituents of the mixture from a) to give an ester mixture, c) isolating the ester of the alkylphosphonous acid from the ester mixture, d) adding the resultant ester of the alkylphosphonous acid onto an olefin containing a functional group. The invention likewise relates to the use of the phosphinic acid esters prepared by this process, inter alia as flame retardants and precursors for further syntheses.

Abstract: Stable, enzymatically triggered chemiluminescent 1,2-dioxetanes with improved water solubility and storage stability are provided as well as synthetic processes and intermediates used in their preparation. Dioxetanes further substituted with two or more water-solubilizing groups disposed on the dioxetane structure and an additional fluorine atom or lower alkyl group provide superior performance by eliminating the problem of reagent carryover when used in assays performed on capsule chemistry analytical systems. These dioxetanes display substantially improved stability on storage. Compositions comprising these dioxetanes, a non-polymeric cationic surfactant enhancer and optionally a fluorescer, for providing enhanced chemiluminescence are also provided.

Abstract: This invention provides analogues of phosphatidylinositol-phosphates modified at one or more selected inositol-hydroxyls and optionally carrying reporter or anchoring groups attached in the lipid or the inositol residues, and, the synthetic intermediates and methods for the preparation of these analogues. The analogues are useful as research reagents in biomedical studies related to structure, function and therapeuticals, including reference materials for analyzing the metabolic products in safety and efficacy studies of 2- and/or 3-hydroxyl modified inositols and phosphatidylinositols as drug candidates.

Abstract: Osteoblast-specific mitogens and drugs containing such compounds can be used for treating metabolic bone diseases. These compounds include lysophosphatidylic acid derivatives selected from the group consisting of compounds of formula: wherein R1=alkenyl or alkynyl having from 6 to 24 carbon atoms; n=0-12; X=oxygen or NH; the compounds (all-cis-5,8,11,14)-eicosatetraenoic acid 2-hydroxy-3-phosphonooxypropyl ester; cis-9, cis-12-octadecadienoic acid 2-hydroxy-3-phosphonooxypropyl ester; (all-cis-9,12,15)-octadecatrienoic acid 2-hydroxy-3-phosphonooxypropyl ester; cis-9-octadecenoic acid 2-hydroxy-3-phosphonooxypropyl ester; and erucic acid 2-hydroxy-3-phosphonooxypropylester being excluded, and the physiologically tolerable salts, esters, optically active forms, and racemates of said compounds, and derivatives of said compounds, salts, esters, optically active forms and racemates which can be metabolized in vivo to yield the corresponding compound of formula (I).

Abstract: The present invention concerns new lipid derivatives of phosphonocarboxylic acids of the general formula I, ##STR1## in which the meaning of the symbols is elucidated in the description, tautomers thereof and their physiologically tolerated esters and salts of inorganic or organic bases as well as processes for the production thereof and pharmaceutical agents containing these compounds.

Abstract: A novel class of anionic surfactants with improved surfact active properties is comprised of two hydrophilic and two hydrophobic groups represented by the formula: ##STR1## The surfactants exhibit unusually low critical micelle concentration (cmc) and pC-20 values in aqueous media.

Abstract: The present invention relates to a process for preparing phosphinic esters which comprisesa) reacting elemental yellow phosphorus with alkyl halides in the presence of alkali metal hydroxide or alkaline earth metal hydroxide to form a mixture which comprises as main constituents the alkali metal salts and/or alkaline earth metal salts of alkylphosphonous acid, phosphorous acid and hypophosphorous acidb) removing the alkylphosphonous acid from the mixture obtained as described in a),c) esterifying the alkylphosphonous acid,d) adding the resultant ester of the alkylphosphonous acid to a compound having at least one C.dbd.C double bond.The invention likewise relates to the use of the phosphinic esters prepared by this process inter alia as flame retardants and as precursor for further syntheses.

Abstract: The present invention relates to phosphonic acid derivatives that inhibit N-Acetylated .alpha.-Linked Acidic Dipeptidase (NAALADase) enzyme activity, pharmaceutical compositions comprising such derivatives, and methods of using such derivatives to inhibit NAALADase activity, to treat a glutamate abnormality and to treat a prostate disease in an animal.

Abstract: This invention relates to compositions for and methods of treating, preventing or ameliorating cancer and other proliferative diseases as well as methods of inducing wound hearing, treating cutaneous ulcers, treating gastrointestinal disorders, treating blood disorders such as anemias, immunomodulation, enhancing recombinant gene expression, treating insulin-dependent patients, treating cystic fibrosis patients, inhibiting telomerase activity, treating virus-associated tumors, especially EBV-associated tumors, modulating gene expression and in particular, augmenting expression of tumor suppressor genes, inducing tolerance to antigens, treating, preventing or ameliorating protozoan infection, or inhibiting histone deacetylase in cells. The compositions of the invention are to and the methods of the invention use oxyalkalene phosphate compounds.

Abstract: Membrane-permeant phosphoinositides, including phosphatidylinositol phosphate esters, are described. A membrane-permeant phosphoinositide includes groups that neutralize the charges of the phosphate moieties of the phosphoinositide. A cell can be treated with the membrane-permeant phosphoinositide, which is then absorbed into the cell. The neutralizing groups can be removed intracellularly to afford the charged phosphoinositide.

Abstract: Phosphites inhibitors for organic material represented by the formula: ##STR1## wherein R.sup.1, R.sup.2, R.sup.4 and R.sup.5 independently represent hydrogen atom, an alkyl group, a cycloalkyl group, an alkylcycloalkyl group, an aralkyl group or a phenyl group; R.sup.3 is hydrogen atom or alkyl; X is a direct bond, sulfur atom, or methylene group which may optionally be substituted with alkyl or cycloalkyl; A represents a dihydric alcohol residue; B is a direct bond or alkylene; and one of Y and Z represents an alkoxy group or an aralkyloxy group, and the other one represents hydrogen atom or an alkyl group; and a process for producing the same are provided.

Abstract: Phosphites which are a deterioration inhibitors for organic material represented by the formula: ##STR1## wherein R.sup.1 and R.sup.2 independently represent a hydrogen atom, or certain hydrocarbyl radicals; X represents a direct bond, a sulfur atom or a methylene group which may optionally be substituted; Z is --A.sup.1 --CO--O--Y.sup.1 or --A.sup.2 --O--CO--Y.sup.2 wherein A.sup.1 is a direct bond or an alkylene group; Y.sup.1 is aralkyl or aryl; A.sup.2 is a residue of a dihydric alcohol; and Y.sup.2 is alkyl, aralkyl or a phenyl group, and a process for producing the same are provided.

Abstract: Compounds of the formula ##STR1## where m and n are integers 0 to 10 and m+n equals 0 to 10, (a) X is O or S(b) Z is a covalent bond; a monocyclic or polycyclic carbocycle ring moiety; or a monocyclic or polycyclic heterocyclic ring moiety containing one or more heteroatoms selected from O, S, or N;(c) Q is covalent bond; O; or S;(d) R is COOH, SO.sub.3 H, PO.sub.3 H.sub.2, or P(O)(OH)R.sup.4, wherein R.sup.4 is C.sub.1 -C.sub.8 alkyl;(e) R.sup.1, R.sup.2 and R.sup.5 are as defined in the claims.are useful in the treatment of calcium and phosphate elated disorders, such as arthritis and the like.

Abstract: The present invention relates to catalytic asymmetric hydrogenation of phosphorus analogs of itaconic acid to synthesize novel optically active phosphono succinates.

Abstract: 1 A process for producing a purified organophosphorus alkyl ester compound in which the reaction mixture obtained by reacting a dichlorophosphine derivative with (meth)acrylic acid is esterified with a lower monool, and the resulting reaction mixture is neutralized with an alkali metal hydroxide or alkaline earth metal hydroxide either in a solid form or in the form of an aqueous solution and purified; 2 a process for producing a purified organophosphorus hydroxyalkyl ester compound or an alkylene glycol solution thereof which comprises subjecting the purified organophosphorus alkyl ester compound obtained by process 1 to transesterification with an alkylene glycol; 3 a reactive flame retardant comprising the purified organophosphorus alkyl ester compound obtained by process 1; and 4 a reactive flame retardant comprising the purified organophosphorus hydroxyalkyl ester compound or alkylene glycol solution obtained by process 2.

Abstract: Inks, particularly inks for ink jet printing, contain at least one compound of the formula I ##STR1## as a stabilizer. The symbols R.sub.1, R.sub.2, R.sub.3, R.sub.4, R.sub.3 ' and R.sub.4 ' are as defined in claim 1. The compounds are in part novel and are suitable for use as light stabilizers for organic materials.

Abstract: A series of compounds of Formula I which have anti-tumor activity, and are useful in treating viral infections, their compositions and use. ##STR1## In Formula I B is a purine or pyrimidine base; alk.sub.1 alk.sub.2 and alk.sub.3 are chemical bonds or alkylene groups; Q is hydrogen or hydroxyl; and R.sub.1 -R.sub.4 are hydrogen or alkyl.

Abstract: Compounds useful in the treatment of inflammation structurally represented as Formula I ##STR1## one of X or Y is H and the other is selected from the group consisting of: ##STR2## or X and Y are taken together to form a ring selected from the group consisting of: ##STR3## as herein defined. The compounds are useful as anti-inflammatory and anti-arthritic agents.

Abstract: New lipopolyamines of general formula (I), their salts, their preparation and their use. ##STR1## n=1 to 5 and m=2 to 6 R represents a radical ##STR2## (R.sub.1 and R.sub.2 : aliphatic radical containing 12 to 22 carbon atoms; R: hydrogen atom or alkyl radical optionally substituted with phenyl), or a radical ##STR3## (X=CH.sub.2, CO; R.sub.3 and R.sub.4 aliphatic radical containing 11 to 21 carbon atoms), their preparation and their use.The lipopolyamines of general formula (I) are especially useful as vectors for the transfection of eukaryotic cells.

Abstract: The present invention provides compounds that function as hydrolytic enzyme inhibitors (inactivators) and substrates. These compounds are useful in assays to detect and measure levels of hydrolytic enzyme activity and are more particularly useful in treatment regimens for various disease states and conditions implicating the underlying specific hydrolytic enzyme. Examples of hydrolytic enzymes include, but are not limited to, phospholipases, lipases, esterases, proteases, etc.

Abstract: Compounds useful in the treatment of inflammation structurally represented as Formula I ##STR1## one of X or Y is H and the other is selected from the group consisting of: ##STR2## or X and Y are taken together to form a ring selected from the group consisting of: ##STR3## as herein defined. The compounds are useful as anti-inflammatory and anti-arthritic agents.

Abstract: A method for the synthesis of a plurality of oligonucleotides comprising the steps of(i) forming a first oligonucleotide on a first cleavable link attached to a solid support;(ii) attaching to the first oligonucleotide a cleavable linker moiety;(iii) forming a second oligonucleotide on the cleavable linker moiety; and(iv) cleaving the first cleavable link and the cleavable linker moiety to give a plurality of oligonucleotides; wherein the cleavable linker moiety is of the Formula (1): ##STR1## in which A.sup.1, A.sup.2 and E are as defined herein, and novel compounds which may be used in the operation of the method.

Abstract: A reaction product useful as an antiwear or antioxidant additive in lubricants is made by reacting a sulfur-containing carboxylic acid, i.e. 3,3'-thiodipropionic acid and a phosphorodithioate, i.e. butoxylated bis(2-ethylhexyl) phosphorodithioic acid.

Abstract: The present invention relates to compounds of the formula I ##STR1## in which R.sup.1 is hydrogen,a substituted or unsubstituted aliphatic radicalhaving up to 30 carbon atoms,a substituted or unsubstituted alicyclic radicalhaving up to 30 carbon atoms,a substituted or unsubstituted aromatic radicalhaving up to 24 carbon atoms ora substituted or unsubstituted heteroaromaticradical having up to 20 carbon atoms,R.sup.2 is an amino acid,x'=0-80,y'=0-50,x"=0-80 andy"=0-50,with at least one of the variables x', y', x" and y" being greater than 0. The compounds of the formula I are prepared by reacting the corresponding dihydrogen phosphate with the respective amino acid or salt thereof. The compounds according to the invention can be employed, for example, as surfactants for emulsifying organic solvents in water.

Abstract: Compounds represented by the formula I: ##STR1## are disclosed as agents for use in treating bone wasting diseases.

Abstract: Phosphoric diesters having formula (1): ##STR1## wherein R.sup.1 is an acyl group having at least one phenyl group; R.sup.2 is a C.sub.2-12 linear or branched alkylene group which may optionally be inserted with an oxygen atom between carbon atoms thereof; L is a C.sub.2-40 linear or branched alkyl group which may optionally be inserted with an oxygen atom between carbon atoms thereof or the group R.sup.1 -O-R.sup.2 ; M is a hydrogen atom, an alkali metal ion, a metal ion of di- or higher valence, an ammonium group, an alkanolammonium group having 2 to 14 carbon atoms, C.sub.1-14 alkylammonium group; and n is the valence of M are useful UV absorbing compounds. The phosphoric diesters remain on the skin for long periods of time and exhibit lasting UV shielding effects. The compounds and the cosmetic compositions containing the compounds are very safe to the skin.

Abstract: The present invention relates to catalytic asymmetric hydrogenation of phosphorus analogs of itaconic acid to synthesize novel optically active phosphono succinates.

Abstract: The present invention provides a phosphorus-containing isoprenoid derivative represented by the following general formula (I) or a pharmacologically acceptable salt thereof, which is useful as a preventive and therapeutic agent for diseases for which a squalene synthetase inhibiting action is efficacious: ##STR1## wherein R.sup.1 and R.sup.2 each represent a hydrogen atom, a lower alkyl, cycloalkyl, alkenyl or alkynyl group, an aryl group which may be substituted, an arylalkyl group in which the aryl group may be substituted, or a heteroaryl or heteroarylalkyl group: R.sup.3 and R.sup.4 each represent a hydrogen atom, a lower alkyl group or an alkali metal; Y represents a group represented by the formula: ##STR2## (wherein R.sup.5 and R.sup.6 each represent a hydrogen atom, a lower alkyl group or an alkali metal or a group represented by the formula: --CO.sub.2 R.sup.7 (wherein R.sup.7 represents a hydrogen atom, a lower alkyl group or an alkali metal); Z represents a group represented by the Formula: --(CH.

Abstract: Substituted cyclohexane derivatives for the treatment of diseases Esters of cyclohexane derivatives of the formula I ##STR1## in which A--B, R.sup.3, R.sup.4, R.sup.5, Y and Z have the meanings indicated, for use as inhibitors of the glucose-6-phosphatase system of the liver in mammals are described. The compounds are suitable for the production of pharmaceutical preparations.

Abstract: Compounds of the formula: ##STR1## which is further defined herein, possess anti-tumor activity.

Abstract: There are disclosed compounds of formula I ##STR1## R.sub.1 and R.sub.2 are each independently of the other C.sub.3 -C.sub.18 alkyl, C.sub.5 -C.sub.12 cycloalkyl, C.sub.5 -C.sub.6 cycloalkylmethyl, C.sub.9 -C.sub.10 bicycloalkylmethyl, C.sub.9 -C.sub.10 tricycloalkylmethyl, phenyl, C.sub.7 -C.sub.6 alkylphenyl or, taken together, are ##STR2## R.sub.3 is hydrogen or methyl, A is ##STR3## R.sub.4 is hydrogen or C.sub.1 -C.sub.6 alkyl, and R.sub.5 is a 5- or 6-membered saturated heterocyclic ring,R.sub.6 is hydrogen or methyl,n is an integer from 1 to 11 and m is an integer from 0 to 4.These compounds are particularly suitable for use as additives for lubricant compositions, hydraulic fluids and machining fluids.

Abstract: A process for the preparation of compounds of formula ##STR1## or salt thereof where R.sub.1 is --X--Z and X is --C.tbd.C--,R.sub.2 and R.sub.2 ' are independently hydrogen, alkyl or trialkylsilyl;R.sub.3 is hydrogen or alkyl; andZ is a hydrophobic anchor;which includes reacting a compound of formula ##STR2## where R.sub.4 is alkyl, cycloalkyl or aryl; and R.sub.5 is trialkylsilyl or triarylsilyl with a compound of formula ##STR3## where Y is a halogen, to form a compound of formula ##STR4## and hydrolyzing the compound of formula IV to obtain the compounds of formula I. Compounds of formula I or salt thereof where R.sub.1 is --OR.sub.2 ' may be prepared by reacting a compound of formula III with a compound of formulaP(OR.sub.2).sub.3.

Abstract: Compounds of the general formula: ##STR1## are useful as surfactants in the preparation of fluorocarbon emulsions, which can be used as oxygen-carrying blood substitutes, and for many other therapeutic and diagnostic applications. They are further useful in liposomal formulations which are themselves therapeutic agents or provide a vehicle for such agents.

Abstract: Compounds of the formula I ##STR1## in which x is 1, 2 or 3, and, if x=1, R.sup.1 is C.sub.1 -C.sub.30 alkyl, C.sub.1 -C.sub.18 alkyl substituted by halogen, --COOR.sup.2, --CN, --NR.sup.3 R.sup.4 or by --CONR.sup.3 R.sup.4, C.sub.2 -C.sub.18 alkyl which is interrupted by --NR.sup.5 --, --O-- or --S--, C.sub.3 -C.sub.18 alkenyl, C.sub.5 -C.sub.12 cycloalkyl, phenyl-C.sub.1 -C.sub.4 alkyl, phenyl which is unsubstituted or substituted by C.sub.1 -C.sub.12 alkyl, halogen, phenyl-C.sub.1 -C.sub.4 alkyl and/or C.sub.1 -C.sub.4 alkoxy, or R.sub.1 is naphthyl, a radical of the formula ##STR2## R.sub.2, R.sub.3, R.sub.4 and R.sub.5, independently of one another, are hydrogen, C.sub.1 -C.sub.18 alkyl, C.sub.5 -C.sub.12 cycloalkyl or phenyl-C.sub.1 -C.sub.4 alkyl, R.sup.6 is hydrogen, methyl, allyl or benzyl, R.sup.7 is hydrogen or --OR.sup.9, R.sup.8 is hydrogen or methyl, R.sup.9 is hydrogen or C.sub.1 -C.sub.30 alkyl, R.sup.10 and R.sup.11, independently of one another, are hydrogen or C.sub.1 -C.sub.

Abstract: .alpha.- Phosphonocarboxylate compounds are provided which inhibit the enzyme squalene synthetase and thereby inhibit cholesterol biosynthesis. These compounds have the formula ##STR1## wherein R.sup.1 is a lipophilic group which contains at least 7 carbons and is substituted alkyl, optionally substituted cycloalkyl, optionally substituted cycloalkylalkyl, optionally substituted alkenyl, optionally substituted alkynyl, optionally substituted arylalkyl or optionally substituted aryl;Z is H, halogen, hydroxy, hydroxyalkyl or lower alkyl;R.sup.2 and R.sup.3 are independently H, metal ion or other pharmaceutically acceptable cation, or a prodrug ester;R.sup.4 is H, metal ion or other pharmaceutically acceptable cation, lower alkyl, lower alkenyl, arylalkyl, aryl or a prodrug ester.

Abstract: The present invention provides compounds that function as hydrolytic enzyme inhibitors (inactivators) and substrates. These compounds are useful in assays to detect and measure levels of hydrolytic enzyme activity and are more particularly useful in treatment regimens for various disease states and conditions implicating the underlying specific hydrolytic enzyme. Examples of hydrolytic enzymes include, but are not limited to, phospholipases, lipases, esterases, proteases, etc.

Abstract: A compound having the formula ##STR1## where X is a radical of myo-inositol or a radical of a configuration isomer thereof where at least one R is ##STR2## where Y is (1) oxygen, (2) a straight or branched alkyl with 1-10 carbon atoms, where Z is ##STR3## where A.sup.1 and A.sup.2 are the same or different and are hydrogen or methyl and n is 3-10, or ##STR4## where A.sup.1 and A.sup.2 are hydrogen or methyl and where m is 1-5, where R.sup.1 is hydrogen, straight or branched alkyl, aryl or alkaryl, alkoxy or aryloxy, where R.sup.2 is(1) R.sup.1,(2) hydroxyl, or(3) OZOCOR.sup.1,and where the remaining R is/are hydroxyl.

Abstract: A process for the preparation of compounds of formula ##STR1## and pharmaceutically acceptable salts thereof; wherein X is --CH.sub.2 --, --CH.sub.2 CH.sub.2 --, --CH.sub.2 CH.sub.2 CH.sub.2 --, --CH.dbd.CH--, --C.tbd.C-- or --CH.sub.2 O-- (where O is linked to Z); Z is a hydrophobic anchor R.sub.1 is hydrogen, alkyl, cycloalkyl or aryl; comprising the steps of:(A) reacting a compound of formula ##STR2## with a compound of formula ##STR3## or a compound of formula ##STR4## in the presence of an amine base or an alkali metal hydride in an organic solvent to form a compound having the formula ##STR5## (B) heating the compound of formula IX at a temperature of from about 100.degree. C. to about 200.degree. C., to form a compound of formula ##STR6## and (C) quenching the compounds of formula VIII with an acid provides the compounds of formula I.

Abstract: The present invention provides triterpene derivatives of the following formula: ##STR1## wherein, R.sup.1 is hydrogen or metabolic ester-residue; R.sup.3 is optionally substituted aryl or optionally substituted aromatic heterocycle; X is hydrogen and Y is hydroxy or X and Y may form together oxo; Z is an oxygen or two hydrogen atoms, or the salts thereof, which have anti-endothelin activities and are useful for preventing or treating cardiovascular failure, and pharmaceutical compositions thereof.

Abstract: Novel phosphorus containing compounds are described, as well as methods for the preparation and pharmaceutical composition of same, which are useful in preventing the intestinal absorption of cholesterol and thus are useful in the treatment of hypercholesterolemia and atherosclerosis.

Abstract: There are disclosed novel compounds of the formula: ##STR1## wherein, x is --CH.sub.2 --, --CHF--, --CF.sub.2, --CHOH-- or --C(O)--;R.sup.6 is hydrogen, benzyl, pentafluorophenyl, nitrophenyl, 1-benzotriazolyl or 1-succinimidoyl;Fmoc is 9-fluorenylmethyloxycarbonyl; and* indicates a chiral carbon atom.The Formula (I) compounds are useful in synthesizing peptides. There are also disclosed novel synthesis methods which include the step of hydrogenating a compound of the Formula ##STR2## wherein R.sup.4 and R.sup.5 are C.sub.1-8 lower alkyl, to give a compound of the formula ##STR3## wherein R.sup.4 and R.sup.5 are as defined above. The compounds of formula (II) are useful as intermediates in preparing certain formula (I) compounds.

Abstract: Process for the preparation of compounds of the formula ##STR1## where R is (C.sub.1 -C.sub.4)alkyl, which comprises reacting a compound of the formula II ##STR2## with an alcoholate of the formula IIIMet-OR (III)where Met is Na or K and R has the abovementioned meaning, at temperature from -30.degree. C. to +10.degree. C.

Abstract: Novel angiotensin II receptor antagonists of the formula ##STR1## wherein X, X.sub.1, X.sub.2, R.sub.1, R.sub.2, R.sub.3, R.sub.4 and R.sub.5 are as defined herein, are disclosed. These compounds are useful, for example, in the treatment of hypertension, congestive heart failure and cardiac hypertrophy.