Abstract:
The present invention relates to a compound of the formula (I) wherein R1 is optionally substituted aryl; R2 is optionally substituted aryl, optionally substituted heteroaryl, optionally substituted lower cycloalkyl, optionally substituted aryloxy, optionally substituted arylsulfonyl, vinyl, carbamoyl, protected carboxy or protected amino; ring A is bivalent residue derived from optionally substituted aryl or optionally substituted heteroaryl; X is bivalent residue derived from the group consisting of cycloalkene, naphthalene, unsaturated 5 or 6-membered heteromonocyclic group, each of which is optionally substituted, and substituted benzene; Y is -(A1)m1-(A2)m2-; and Z is direct bond or piperazine, or a salt thereof. The compound of the present invention and a salt thereof inhibit apolipoprotein B (Apo B) secretion and are useful as a medicament for prophylactic and treatment of diseases or conditions resulting from elevated circulating levels of Apo B.
Abstract:
A process for producing an erythro-3-amino-2-hydroxybutyric acid derivative characterized in that an erythro-3-amino-2-hydroxybutyronitrile derivative represented by the general formula [II] (wherein R 1 is a straight-chain, branched or cyclic alkyl group having one to six carbon atoms, an alkylthio group or an arylthio group having one to eight carbon atoms, or a substituted or unsubstituted aryl group, P 1 and P 2 are, the same or different, a substituted or unsubstituted aralkyl group, a substituted or unsubstituted aralkyloxycarbonyl group, a substituted or unsubstituted arylcarbonyl group, or a substituted or unsubstituted arylsulfonyl group, and R 2 is an alkylcarbonyl group, or a substituted or unsubstituted arylcarbonyl group), is treated with an acid in water or in a water-containing solvent to convert it into an erythro-3-amino-2-hydroxybutyric acid derivative represented by the general formula [III] (wherein R 1 is the same as mentioned above, R 3 is hydrogen, Q 1 and Q 2 are, the same or different, hydrogen, a substituted or unsubstituted aralkyl group, or a substituted or unsubstituted arylsulfonyl group), or the nitrile derivative is treated with an acid in an alcoholic solvent represented by the general formula of R 3 OH to convert it into an ester of the butyric acid represented by the above general formula [III] (R 3 is a straight-chain, branched or cyclic alkyl group having one to six carbon atoms, or a substituted or unsubstituted aralkyl group).
Abstract:
A process for preparing an optically active 4-halogeno-l,3-butanediol and (R)-1,2,4-butanetriol or (S)-3-hydroxy-y-butyrolactone which comprises reacting a racemic 4-halogeno-1,3-butanediol with a specific microorganism belonging to the genus Pseudomonas.
Abstract:
An improved process for producing 4-hydroxy-2-pyrrolidone represented by formula (1), which is useful as an intermediate for synthesizing medicines, agricultural chemicals and so forth, by synthesizing a 4-azido-3-hydroxybutanoic ester by the reaction of a 4-halogeno-3-hydroxybutanoic ester with an alkali metal or alkaline earth metal azide followed by the catalytic reduction of the azido group of the ester and cyclization.
Abstract:
A process for preparation of (R)-1,2-propanediol which comprises cultivating a microorganism belonging to genus Pseudomonas or genus Alcaligenes which has ability to assimilate (S)-1,2-propanediol as a single carbon source, in a culture medium containing racemic 1,2-propanediol as a single carbon source and then isolating the remaining (R)-1,2-propanediol from the culture broth.
Abstract:
A process for the preparation of an optically active 1,2-diol compound of the following formula: wherein R is an alkyl group, hydroxy substituted alkyl group, or alkenyl group, which comprises reacting a corresponding racemic 1,2-diol compound with a strain belonging to the genus Alcaligenes which is cultivated under aeration.
Abstract:
A process for preparing 1,3-dioxolane-4-methanol compounds in a racemic modification form and an optically active form having a high purity in a high yield in a simple and cost-effective manner. The process comprises reacting a 3-halogeno-1,2-propanediol (1a) (wherein X represents a halogen atom) or a glycidol with an alcohol in the presence of a base, acetalating the resultant 3-alkoxy-1,2-propanediol in the presence of an acid catalyst, and further conducting hydrogenation in the presence of a reduction catalyst to prepare a 1,3-dioxolane-4-methanol compound (5) (wherein R?1 and R2¿ represent each hydrogen, an alkyl group having 1 to 4 carbon atoms, or a phenyl group, or R?1 and R2¿ together with the adjacent carbon atom may form a three- to six-membered ring).