C07D309/06

Kinetic resolution of racemic hydroxy ester via asymmetric catalytic hydrogenation and application thereof
20170334831 · 2017-11-23 ·

The present invention relates to kinetic resolution of racemic δ-hydroxyl ester via asymmetric catalytic hydrogenation and an application thereof. In the presence of chiral spiro pyridyl phosphine ligand Iridium catalyst and base, racemic δ-hydroxyl esters were subjected to asymmetric catalytic hydrogenation to obtain extent optical purity chiral δ-hydroxyl esters and corresponding 1,5-diols. The method is a new, efficient, highly selective, economical, desirably operable and environmentally friendly method suitable for industrial production. An optically active chiral δ-hydroxyl ester and 1,5-diols can be obtained at very high enantioselectivity and yield with relatively low usage of catalyst. The chiral δ-hydroxyl ester and 1,5-diols obtained by using the method can be used as a critical raw material for asymmetric synthesis of chiral drugs (R)-lisofylline and natural drugs (+)-civet, (−)-indolizidine 167B and (−)-coniine.

Kinetic resolution of racemic hydroxy ester via asymmetric catalytic hydrogenation and application thereof
20170334831 · 2017-11-23 ·

The present invention relates to kinetic resolution of racemic δ-hydroxyl ester via asymmetric catalytic hydrogenation and an application thereof. In the presence of chiral spiro pyridyl phosphine ligand Iridium catalyst and base, racemic δ-hydroxyl esters were subjected to asymmetric catalytic hydrogenation to obtain extent optical purity chiral δ-hydroxyl esters and corresponding 1,5-diols. The method is a new, efficient, highly selective, economical, desirably operable and environmentally friendly method suitable for industrial production. An optically active chiral δ-hydroxyl ester and 1,5-diols can be obtained at very high enantioselectivity and yield with relatively low usage of catalyst. The chiral δ-hydroxyl ester and 1,5-diols obtained by using the method can be used as a critical raw material for asymmetric synthesis of chiral drugs (R)-lisofylline and natural drugs (+)-civet, (−)-indolizidine 167B and (−)-coniine.

NOVEL IMAGING COMPOSITION AND USES THEREOF

The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours.

NOVEL IMAGING COMPOSITION AND USES THEREOF

The invention discussed in this application relates to hydroxamic acid-based compounds that are useful as imaging agents when bound to an appropriate metal centre, particularly for the imaging of tumours.

BIS(SULFONAMIDE) DERIVATIVES AND THEIR USE AS MPGES INHIBITORS

The present invention relates to bis(sulfonamide) compounds and pharmaceutically acceptable salts thereof. The present invention also relates to pharmaceutical compositions comprising these compounds and to their use as a medicament for the treatment and/or prevention of a disease, disorder or condition in which modulation of microsomal prostaglandin E synthase-1 activity is beneficial, such as pain, inflammation and cancer.

BIS(SULFONAMIDE) DERIVATIVES AND THEIR USE AS MPGES INHIBITORS

The present invention relates to bis(sulfonamide) compounds and pharmaceutically acceptable salts thereof. The present invention also relates to pharmaceutical compositions comprising these compounds and to their use as a medicament for the treatment and/or prevention of a disease, disorder or condition in which modulation of microsomal prostaglandin E synthase-1 activity is beneficial, such as pain, inflammation and cancer.

Carbonyl derivative, liquid crystal composition containing compound thereof and liquid crystal display device

To provide a liquid crystal compound satisfying at least one of physical properties such as a high stability to heat, light and so forth, a high clearing point, a low minimum temperature of a liquid crystal phase, a small viscosity, a suitable optical anisotropy, a large dielectric anisotropy, a suitable elastic constant and an excellent compatibility with other liquid crystal compounds; a liquid crystal composition containing the compound; and a liquid crystal display device including the composition. The compound is represented by formula (1): ##STR00001##
wherein, for example, Ra and Rb are alkyl having 1 to 10 carbons, alkenyl having 2 to 10 carbons or alkoxy having 1 to 9 carbons; A.sup.1, A.sup.2 and A.sup.3 are 1,4-cyclohexylene or 1,4-phenylene; Z.sup.1 and Z.sup.2 are single bonds, —(CH.sub.2).sub.2—, —CH═CH—, —COO—, —OCO—, —CF.sub.2O—, —OCF.sub.2—, —CH.sub.2O— or —OCH.sub.2—; Y.sup.1 is —CF.sub.2H or —CF.sub.3; Y.sup.2 is fluorine; and a, b and d are 0, 1, 2 or 3, and c is 1 or 3.

Carbonyl derivative, liquid crystal composition containing compound thereof and liquid crystal display device

To provide a liquid crystal compound satisfying at least one of physical properties such as a high stability to heat, light and so forth, a high clearing point, a low minimum temperature of a liquid crystal phase, a small viscosity, a suitable optical anisotropy, a large dielectric anisotropy, a suitable elastic constant and an excellent compatibility with other liquid crystal compounds; a liquid crystal composition containing the compound; and a liquid crystal display device including the composition. The compound is represented by formula (1): ##STR00001##
wherein, for example, Ra and Rb are alkyl having 1 to 10 carbons, alkenyl having 2 to 10 carbons or alkoxy having 1 to 9 carbons; A.sup.1, A.sup.2 and A.sup.3 are 1,4-cyclohexylene or 1,4-phenylene; Z.sup.1 and Z.sup.2 are single bonds, —(CH.sub.2).sub.2—, —CH═CH—, —COO—, —OCO—, —CF.sub.2O—, —OCF.sub.2—, —CH.sub.2O— or —OCH.sub.2—; Y.sup.1 is —CF.sub.2H or —CF.sub.3; Y.sup.2 is fluorine; and a, b and d are 0, 1, 2 or 3, and c is 1 or 3.

Liquid crystal display device and liquid crystal composition used therefor

A liquid crystal display device comprises a first substrate, a second substrate which faces the first substrate, an electrode part which is provided on at least one of the first substrate and the second substrate, and a liquid crystal layer which comprises a liquid crystal composition and is provided between the first substrate and the second substrate. The liquid crystal composition includes a liquid crystal compound of Formula 1. ##STR00001##
wherein R.sub.1, R.sub.2, A.sub.11, A.sub.12, A.sub.13, A.sub.21, A.sub.22, Z.sub.11, Z.sub.12, Z.sub.13, Z.sub.21, Z.sub.22, a, b, c, d, and e are as described herein.

Liquid crystal display device and liquid crystal composition used therefor

A liquid crystal display device comprises a first substrate, a second substrate which faces the first substrate, an electrode part which is provided on at least one of the first substrate and the second substrate, and a liquid crystal layer which comprises a liquid crystal composition and is provided between the first substrate and the second substrate. The liquid crystal composition includes a liquid crystal compound of Formula 1. ##STR00001##
wherein R.sub.1, R.sub.2, A.sub.11, A.sub.12, A.sub.13, A.sub.21, A.sub.22, Z.sub.11, Z.sub.12, Z.sub.13, Z.sub.21, Z.sub.22, a, b, c, d, and e are as described herein.