A hydrophilic polymer derivative having a cyclic benzylidene acetal linker represented by the following formula (1): ##STR00001##
wherein R.sup.1 and R.sup.6 are each independently a hydrogen atom or a hydrocarbon group; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each independently an electron-withdrawing or electron-donating substituent or a hydrogen atom; X.sup.1 is a chemically reactive functional group; P is a hydrophilic polymer; s is 1 or 2, t is 0 or 1, and s+t is 1 or 2; w is an integer of 1 to 8; and Z.sup.1 and Z.sup.2 are each independently a selected divalent spacer.

A hydrophilic polymer derivative having a cyclic benzylidene acetal linker represented by the following formula (1): ##STR00001##
wherein R.sup.1 and R.sup.6 are each independently a hydrogen atom or a hydrocarbon group; R.sup.2, R.sup.3, R.sup.4 and R.sup.5 are each independently an electron-withdrawing or electron-donating substituent or a hydrogen atom; X.sup.1 is a chemically reactive functional group; P is a hydrophilic polymer; s is 1 or 2, t is 0 or 1, and s+t is 1 or 2; w is an integer of 1 to 8; and Z.sup.1 and Z.sup.2 are each independently a selected divalent spacer.

The invention relates to a method for the preparation of a 4,5-dihydroxyisoleucine derivative comprising the steps of asymmetric Claisen rearrangement of a Z-aminocrotyl-glycin ester and subsequent kinetic resolution of the product diastereomer mix by acylase, and subsequent Sharpless dihydroxylation of the resulting 2-amino-3-methylpent-4-enoic acid derivative.

Compositions and methods for repelling arthropods. The compositions include a carrier and an arthropod repelling compound, which can be a compound discovered by a novel and complex cheminformatic process to demonstrate repellency behavior across a broad spectrum of arthropods. The compound can be a thiane compound, a pyrrolidone compound, a cyclohexadiene compound, a cyclohexenone compound, a cyclohexene compound, a furanone compound, a pyran compound, a tetrahydropyran compound, a thiazolidine compound, a thiazoline compound, a dihydrothiophene compound, a dithiolane compound, a dithiane compound, an epoxide compound, an oxathiane compound, a cyclopentene compound, a cyclohexane compound, a quinoline compound, an oxazoline compound, a tetrahydropyridine compound, and an imidazolidinone compound, or a combination thereof.

Compositions and methods for repelling arthropods. The compositions include a carrier and an arthropod repelling compound, which can be a compound discovered by a novel and complex cheminformatic process to demonstrate repellency behavior across a broad spectrum of arthropods. The compound can be a thiane compound, a pyrrolidone compound, a cyclohexadiene compound, a cyclohexenone compound, a cyclohexene compound, a furanone compound, a pyran compound, a tetrahydropyran compound, a thiazolidine compound, a thiazoline compound, a dihydrothiophene compound, a dithiolane compound, a dithiane compound, an epoxide compound, an oxathiane compound, a cyclopentene compound, a cyclohexane compound, a quinoline compound, an oxazoline compound, a tetrahydropyridine compound, and an imidazolidinone compound, or a combination thereof.

The present invention aims to provide a method of producing, more efficiently at a high purity, a phosphoramidite preferable for the production (synthesis) of a nucleic acid. Using a coupling reaction of an ether represented by the following chemical formula (105), an enantiomer, tautomer or stereoisomer thereof, or a salt thereof, and a glycoside compound, phosphoramidite that enables efficient synthesis of nucleic acid can be obtained:

##STR00001##

wherein n is a positive integer, and R and R′ are the same or different and each is a hydrogen atom or a hydroxyl-protecting group.

The present invention aims to provide a method of producing, more efficiently at a high purity, a phosphoramidite preferable for the production (synthesis) of a nucleic acid. Using a coupling reaction of an ether represented by the following chemical formula (105), an enantiomer, tautomer or stereoisomer thereof, or a salt thereof, and a glycoside compound, phosphoramidite that enables efficient synthesis of nucleic acid can be obtained:

##STR00001##

wherein n is a positive integer, and R and R′ are the same or different and each is a hydrogen atom or a hydroxyl-protecting group.

A method for manufacturing solketal ((2,2-Dimethyl-1,3-dioxolan-4-yl)methanol) includes: (1) milling starting reagents, including at least: glycerol, a catalyst selected from a hard Lewis acid including at least one transition metal, and acetone, the molar ratio (glycerol):(acetone) being less than or equal to 0.8; preferably less than or equal to 0.7, at an ambient temperature greater than or equal to 50° C., preferably greater than or equal to 56° C., in a three-dimensional microbead mill in a liquid phase for a residence time less than or equal to 15 minutes, preferably less than or equal to 10 minutes, and in particular less than or equal to 5 minutes; (2) recovering, as output from the mill, a final composition including solketal and, where appropriate, one or more sub-products corresponding to the starting reagents that have not reacted and/or to 1,3-O-isopropylidene-glycerol, and (3) optionally, separating the solketal from the one or more sub-products.

A method for manufacturing solketal ((2,2-Dimethyl-1,3-dioxolan-4-yl)methanol) includes: (1) milling starting reagents, including at least: glycerol, a catalyst selected from a hard Lewis acid including at least one transition metal, and acetone, the molar ratio (glycerol):(acetone) being less than or equal to 0.8; preferably less than or equal to 0.7, at an ambient temperature greater than or equal to 50° C., preferably greater than or equal to 56° C., in a three-dimensional microbead mill in a liquid phase for a residence time less than or equal to 15 minutes, preferably less than or equal to 10 minutes, and in particular less than or equal to 5 minutes; (2) recovering, as output from the mill, a final composition including solketal and, where appropriate, one or more sub-products corresponding to the starting reagents that have not reacted and/or to 1,3-O-isopropylidene-glycerol, and (3) optionally, separating the solketal from the one or more sub-products.

Compositions and methods for repelling arthropods. The compositions include a carrier and an arthropod repelling compound, which can be a compound discovered by a novel and complex cheminformatic process to demonstrate repellency behavior across a broad spectrum of arthropods. The compound can be a thiane compound, a pyrrolidone compound, a cyclohexadiene compound, a cyclohexenone compound, a cyclohexene compound, a furanone compound, a pyran compound, a tetrahydropyran compound, a thiazolidine compound, a thiazoline compound, a dihydrothiophene compound, a dithiolane compound, a dithiane compound, an epoxide compound, an oxathiane compound, a cyclopentene compound, a cyclohexane compound, a quinoline compound, an oxazoline compound, a tetrahydropyridine compound, and an imidazolidinone compound, or a combination thereof.