Abstract: The present invention provides novel compounds useful as proteasome inhibitors. The invention also provides pharmaceutical compositions comprising the compounds of the invention and methods of using the compositions in the treatment of various diseases.

Abstract: A compound includes a boron atom attached to at least one C8-C26 fatty acid residue having at least one C?C moiety. Such compounds are polymerizable through the at least one C?C moiety. Polymers thus formed exhibit anti-fouling properties when used as coatings.

Abstract: Provided are a salt compound, cationic polymerization initiator and cationically polymerizable composition, which have a superior acid-generating capacity and high sensitivity, and are free from coloration. The salt compound is represented by the following general Formula (1): (wherein, R01 to R05 each independently represents a group selected from a hydrogen atom, a fluorine atom and —YR group, one of the R01 to R05 being a —YR group and at least two of the R01 to R05 being fluorine atoms; Y represents an oxygen atom or a sulfur atom; R represents a C1-C4 alkyl group; Ctp+ represents a p-valent cation, the p being 1 or 2; and n represents a coefficient required for maintaining electrical neutrality).

Abstract: The present invention relates to new borane complexes with substituted pyridines, a process for the synthesis of new borane complexes with substituted pyridines, solutions comprising new borane complexes with substituted pyridines and a method of using new borane complexes with substituted pyridines for organic reactions.

Abstract: The present invention features a chemoselective ligation reaction that can be carried out under physiological conditions. In general, the invention involves condensation of a specifically engineered phosphine, which can provide for formation of an amide bond between the two reactive partners resulting in a final product comprising a phosphine moiety, or which can be engineered to comprise a cleavable linker so that a substituent of the phosphine is transferred to the azide, releasing an oxidized phosphine byproduct and producing a native amide bond in the final product. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

Abstract: The present invention provides a method for industrial production of trihydrocarbylborane which method is excellent both in quality and in cost. The present invention is concerned with production of trihydrocarbylborane, comprising a reaction synthesizing the trihydrocarbylborane and aluminum oxide from trihydrocarbylboroxine and trihydrocarbylaluminum, characterized in that the reaction is allowed to proceed so that the trihydrocarbylaluminum is present at the end of the reaction in an amount of 0.5 moles or more per mole of the aluminum oxide produced in the reaction.

Abstract: The dental adhesive composition of the present invention comprises a polyfunctional polymerizable monomer which is an ester compound of a polyhydric alcohol of 3 to 6 carbon atoms and plural (meth)acrylic acids and has 1 to 2 hydroxyl groups, a monofunctional (meth)acrylate having no hydroxyl group in its molecule, a polymerizable monomer containing an acid group in its molecule, an organoboron compound as a curing agent and a filler. According to the present invention, a dental adhesive composition remarkably enhanced in the curing rate with rarely affecting adhesion properties of the composition, working time and flexibility of a cured product is provided.

Abstract: The present invention provides a method for industrial production of trihydrocarbylborane which method is excellent both in quality and in cost. The present invention is concerned with production of trihydrocarbylborane, comprising a reaction synthesizing the trihydrocarbylborane and aluminum oxide from trihydrocarbylboroxine and trihydrocarbylaluminum, characterized in that the reaction is allowed to proceed so that the trihydrocarbylaluminum is present at the end of the reaction in an amount of 0.5 moles or more per mole of the aluminum oxide produced in the reaction.

Abstract: Non-coordinating anions or anion precursors are disclosed. These non-coordinating anions serve as the activator for olefin polymerization catalyst systems. As such, they abstract an alkyl leaving group from a metallocene catalyst precursor leaving an activated catalyst charge balanced by a non-coordinating anion. These anions are formed by 3 or 4 partially fluorinated naphthyl ligands coordinated around boron (or other Group-13 element) creating corresponding tris-borane or tetrakis-borate complexes.

Abstract: A method of purifying an organometallic compound by heating the organometallic compound in the presence of a trialkyl aluminum compound and a catalyst.

Abstract: The present invention features a chemoselective ligation reaction that can be carried out under physiological conditions. In general, the invention involves condensation of a specifically engineered phosphine, which can provide for formation of an amide bond between the two reactive partners resulting in a final product comprising a phosphine moiety, or which can be engineered to comprise a cleavable linker so that a substituent of the phosphine is transferred to the azide, releasing an oxidized phosphine byproduct and producing a native amide bond in the final product. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

Abstract: A process for preparing bisallylboranes of the formula (I) by reacting a diene with sodium borohydride in the presence of an oxidant: in an inert solvent, with the borane generated in situ reacting selectively with the diene to form the bis(allyl)borane of the formula (I) and the substituents R1 to R6 having the following meanings: R114 R6 are H, aryl or substituted or unsubstituted C1-C4-alkyl or two radicals R may be closed to form a cyclic system. As oxidant, it is possible to use, for example, alkyl halides or dialkyl sulfates. In a particularly preferred embodiment, the diene used is 2,5-dimethylhexa-2,4-diene (R1, R2, R5, R6=methyl, R3, R4=H).

Abstract: The invention is an amine-organoborane complex wherein the organoborane is a trialkyl borane and the amine is an amine having an amidine structural component; an aliphatic heterocycle having at least one nitrogen in the heterocyclic ring wherein the heterocyclic compound may also contain one or more nitrogen atoms, oxygen atoms, sulfur atoms, or double bonds in the heterocycle; a primary amine which in addition has one or more hydrogen bond accepting groups wherein there is at least two carbon atoms, preferably three, between the primary amine and the hydrogen bond accepting group, such that due to inter- or intramolecular interactions within the complex the strength of the B—N bond is increased; or a conjugated imine. Preferred hydrogen bond accepting groups include the following: a secondary amine, a tertiary amine, an ether, a halogen, a polyether group or a polyamine group.

Abstract: The present invention relates to novel chiral 1,1′-ferrocenylene diphosphonites and the synthesis thereof, in addition to complexes of said compounds with metals from groups VIIb, VIIIb and Ib of the Periodic Table and to the use thereof for enantioselective hydrogenation of olefins, ketones and imines, or enantioselective hydroboration and 1,4-addition to activated olefins.

Abstract: The present invention features a chemoselective ligation reaction that can be carried out under physiological conditions. In general, the invention involves condensation of a specifically engineered phosphine, which can provide for formation of an amide bond between the two reactive partners resulting in a final product comprising a phosphine moiety, or which can be engineered to comprise a cleavable linker so that a substituent of the phosphine is transferred to the azide, releasing an oxidized phosphine byproduct and producing a native amide bond in the final product. The selectivity of the reaction and its compatibility with aqueous environments provides for its application in vivo (e.g., on the cell surface or intracellularly) and in vitro (e.g., synthesis of peptides and other polymers, production of modified (e.g., labeled) amino acids).

Abstract: The invention relates to the combinatorial approaches to the preparation of novel polymer-supported heteroatom bidentate (PN, PO, PS) ligand libraries and the corresponding free compounds after cleavage from the supports. These compounds are useful as novel ligands in the preparation of metal-containing catalysts.

Abstract: A synthetic route for forming lithium trisubstituted borohydride compounds comprises the step of reacting a processed lithium hydride reactant with a trisubstituted borane wherein the reaction is maintained for a period of time in a temperature range of approximately 15° C. to approximately 42° C. A method of synthesizing LiH comprises the step of reacting an alkyl lithium (for example, n-butyl lithium) with hydrogen in the presence of tetrahydrofuran. The reaction temperature is preferably maintained in the range of approximately −78° C. to approximately 25° C.

Abstract: A polymerization initiator composition comprising 100 parts by weight of an organic boron compound (A) and 10 to 150 parts by weight of an aprotic solvent (B) having a boiling point of 30 to 150.degree. C.; and a dental or surgical adhesive composition containing the above polymerization initiator composition.

Abstract: A compound of the general formula:A-L.sup.+ D.sup.-where A is a moiety which absorbs radiation and enters an excited state in which it accepts an electron; D.sup.- is a moiety which donates an electron to the excited state A and releases a free radical; and L.sup.+ is a cationic linking group which tethers electron acceptor moiety A to electron donor moiety D.sup.-. Cationic linking moiety L.sup.+ has the formula:-L'-G-where L' is a moiety which forms a stable radical with acceptor moiety A upon transfer of an electron from donor moiety D.sup.- to electron acceptor moiety A, and G is a moiety which forms a leaving group upon transfer of the electron from donor moiety D.sup.- to acceptor moiety A.

Abstract: Synthetic routes for forming alkali metal substituted borohydride compounds include the step of reacting an alkali metal reagent, a hydrogen donor, and a substituted borane. The reactions proceed without the requirement of specialized handling of alkali metal hydrides associated with prior synthetic processes for the production of alkali metal trisubstituted borohydride compounds. A chemical composition comprises solid potassium tri-sec-butyl borohydride.

Abstract: A compound having the formula: ##STR1## where A.sup.- is a counterion; R.sup.1, R.sup.2, R.sup.3, and R.sup.4, independently, comprise (a) a non-fluorinated alkyl, cycloalkyl, aryl, or aralkyl group; (b) an onium-containing group; or (c) a group having the formula --(CH.sub.2).sub.n --Y--R.sup.5 in which n is at least two; Y is a spacer arm comprising a --CH.sub.2 --, --O--, --OCH.sub.2 --, --S--, --SO.sub.2 --, or --Z--SO.sub.2 -- group; Z is an --R.sup.6 --O--, --N(R.sup.7)-- group, or --N(H)--; R.sup.6 is a substituted or unsubstituted phenylene group; R.sup.7 is H or a non-fluorinated alkyl, cycloalkyl, aryl, or alkaryl group; and R.sup.5 is a fluorinated group, perfluorinated group, or combination thereof, with the proviso that (i) at least one of R.sup.1, R.sup.2, R.sup.3, and R.sup.4 comprises a group having the formula --(CH.sub.2).sub.n --Y--R.sup.5 ; and (ii) the total number of fluorine atoms in said compound is at least 5.

Abstract: Novel onium borates of an element of Groups 15 to 17 of the Periodic Table, or borates of an organometallic complex of an element of Groups 4 to 10 of the Periodic Table, well suited for the photochemical/electron beam cationic initiation of polymerization/crosslinking, the anionic borate moiety of which having the formula:[BX.sub.a R.sub.b ].sup.-in which a and b are integers ranging from 0 to 4 and a+b=4; the symbols X are each a halogen atom when a ranges up to 3 and an OH functional group when a ranges up to 2; and the symbols R, which may be identical or different, are each a phenyl radical substituted by at least one element or electron-withdrawing substituent or by at least two halogen atoms, or an aryl radical containing at least two aromatic ring members, or such aryl radical bearing at least one electron-withdrawing substituent.

Abstract: Metallocene complexes of the general formula I ##STR1## where the substituents Y, M, x, R.sup.1, R.sup.2, R.sup.3, R.sup.4, R.sup.6, R.sup.7, R.sup.8, and R.sup.9 are as described in the disclosure, and ligand systems of the general formula II ##STR2## as intermediates.

Abstract: Process for the preparation of trialkyl compound of a Group 3a metal, in which a Group 3a metal is contacted with an alkyl halide in the presence of an alkali metal to obtain a trialkyl compound of the Group 3a metal and alkali-metal halide.

Abstract: Novel onium borates of an element of Groups 15 to 17 of the Periodic Table, or borates of an organometallic complex of an element of Groups 4 to 10 of the Periodic Table, well suited for the photochemical/electron beam cationic initiation of polymerization/crosslinking, the anionic borate moiety of which having the formula:[BX.sub.a R.sub.b ].sup.-in which a and b are integers ranging from 0 to 4 and a+b=4; the symbols X are each a halogen atom when a ranges up to 3 and an OH functional group when a ranges up to 2; and the symbols R, which may be identical or different, are each a phenyl radical substituted by at least one element or electron-withdrawing substituent or by at least two halogen atoms, or an aryl radical containing at least two aromatic ring members, or such aryl radical bearing at least one electron-withdrawing substituent.

Abstract: The present invention relates to a process for the synthesis of chiral enantiomerically pure .beta.-amino alcohols which are extraordinarily important as therapeutic agents for the treatment of a variety of human disorders and as chiral auxiliaries in organic synthesis. The hydroboration of enamines is a versatile and convenient method for the synthesis of both racemic and enantiomerically pure .beta.-amino alcohols in high yields. This methodology enables the synthesis of virtually any .beta.-amino alcohol. Hydroboration of these enamines with chiral organic borohydrides, e.g. either mono- or diisopinocampheylborane, followed by oxidation with aqueous or solid NaOH/30% H.sub.2 O.sub.2 or Me.sub.3 NO, gives the corresponding chiral .beta.-amino alcohol. Enantiomeric excesses ranged from 60% for reactions run at 25.degree. C. to greater than 99% for reactions run at -25.degree. C.

Abstract: A novel process for producing hindered and unhindered primary amines represented by the formula RNH.sub.2 and R*NH.sub.2 in high yields from novel intermediates RBMe.sub.2 or R*BMe.sub.2 wherein R is an organo group, R* is a chiral organo group. attached to boron, B is boron and Me is methyl.

Abstract: A process for preparing a dimethylorganoborane represented by the formula R*BMe.sub.2 wherein R* is a chiral organyl group attached to the boron, B is boron and Me is methyl comprising treating a chiral boronic ester R*B(OR').sub.2 with a methyl magnesium salt or trimethylaluminum wherein R* is the same chiral organyl group and R' is alkyl.

Abstract: A novel process for producing hindered and unhindered primary amines represented by the formula RNH.sub.2 and R*NH.sub.2 in high yields from novel intermediates RBMe.sub.2 or R*BMe.sub.2 wherein R is an organo group, R* is a chiral organo group,attached to boron, B is boron and Me is methyl.

Abstract: A novel process for producing hindered and unhindered primary amines represented by the formula RNH.sub.2 and R*NH.sub.2 in high yields from novel intermediates RBMe.sub.2 or R*BMe.sub.2 wherein R is an organo group, R* is a chiral organo group, attached to boron, B is boron and Me is methyl.

Abstract: Methods for forming or purifying organometallic compounds of elements of Group III-A of the Periodic Table. An intermediate compound is formed which is an adduct of the desired organometallic compound and a Group I-A or Group II-A compound. The adduct is nonvolatile, so volatile impurities are removed from the adduct by distillation. The adduct is decomposed to release the volatile organometallic compound, which is then distilled away from the nonvolatile remainder of the adduct. The method can be used to produce organometallic compounds which are substantially free of volatile metallic compounds and complexed solvents. A method of separating volatile Group II-B impurities from volatile Group III-A compounds is also disclosed.

Abstract: A process for upgrading to essentially 100% enantiomeric excess the optical purity of an organoborane intermediate represented by the formulae:IcpBHR*orIcp.sub.2 BR*wherein Icp is isopinocampheyl and R* is a unsubstituted or substituted, acyclic or cyclic alkyl having from 4 to 30 carbon atoms, comprising the steps of hydroborating cis-alkene, a trans-alkene or a tertiary-alkene with monoisopinocampheylborane or diisopinocampheylborane, obtaining a solid organoborane and recrystallizing the solid organoborane to obtain an enantiomeric excess of essentially 100% ee of said organoborane.

Abstract: Process for the production of the insect sex attractant, gossyplure, is provided. The process comprises first disproportionating 1,5-cyclooctadiene and 1-hexene to give 1,5,9-tetradecatriene, then metallating the triene to form a 1-metallo-5,9-tetradecadiene, and finally treating the organometal compound with a C.sub.2 -synthon to give directly 7,11-hexadecadienyl acetate or a substituted 7,11-hexadecadienyl moiety which can readily be converted to the desired acetate.

Abstract: Process for the production of the insect sex attractant, gossyplure, is provided. The process comprises first disproportionating 1,5-cyclooctadiene and 1-hexene to give 1,5,9-tetradecatriene, then metallating the triene to form a 1-metallo-5,9-tetradecadiene, and finally treating the organometal compound with a C.sub.2 -synthon to give directly 7,11-hexadecadienyl acetate or a substituted 7,11-hexadecadienyl moiety which can readily be converted to the desired acetate.

Abstract: Agglomeration of dispersions of an alkali metal in an organic liquid is reduced by adding at least about 2.5% of an aryl halide, e.g., chlorobenzene.

Abstract: Agglomeration of dispersions of an alkali metal in an organic liquid is reduced by adding at least about 2.5% of an aryl halide, e.g., chlorobenzene.

Abstract: The novel borane-1,4-thioxane is synthesized by adding the calculated quantity of diborane to 1,4-thioxane. It is a stable liquid at 25.degree. C. The neat liquid is approximately 8.0 M in borane. The product, in spite of the additional oxygen atom in the ring, exhibits the desirable hydroborating and reducing action of borane-methyl sulfide. However, it possesses a major advantage over the latter in that the donor component, 1,4-thioxane, in contrast to methyl sulfide, is readily soluble in water and can be washed out of typical reaction mixtures. This greatly facilitates the synthetic applications of borane-1,4-thioxane over borane-methyl sulfide.

Abstract: An adhesive which comprises aqueous and nonaqueous polymers suitable for holding an lipophilic drug, etc., and has tackiness and cohesiveness which are sufficient for the plaster of a patch; and a patch employing the adhesive. The adhesive contains a polymer which comprises one or more kinds of acrylic or methacrylic monomer units, at least one kind of the monomer units having a hydroxy group, and which has been crosslinked with a boron compound.