摘要:
It is an objective of the present invention to provide a means for producing rapidly soluble granules with the use of any powdery raw material that is poorly sedimented in water and thus is dispersed or dissolved with difficulty in water.According to the present invention, a method for producing rapidly soluble granules, comprising mixing granules having poor sedimentation property in water and granules having good sedimentation property in water while adding an emulsifier thereto to thereby obtain mixed granules coated with the emulsifier.
摘要:
The present invention relates a process for producing the quinoline derivative (3) via the nitrile compound (1) obtained by reacting the aldehyde compound represented by formula (2) with diethyl cyanomethylphosphonate and its intermediate (1).
摘要:
A method for producing a drug substance of crystalline pitavastatin calcium excellent in stability, is presented. In the production of a compound (pitavastatin calcium) represented by the formula (1): The water content is adjusted to a level of from 5 to 15%, and the crystal form is controlled to be crystal form A, thereby to obtain a drug substance excellent in stability.
摘要:
An optically active .beta.-aminoalkoxyborane complex of the formula (I): ##STR1## wherein R.sup.1 is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.7 -C.sub.11 aralkyl or C.sub.6 -C.sub.10 aryl, R.sup.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.7 cycloalkyl or C.sub.7 -C.sub.11 aralkyl, or R.sup.1 and R.sup.2 together form (CH.sub.2).sub.n wherein n is 3 or 4, and Ar is naphthyl, anthryl or phenanthryl, which may be substituted by from 1 to 3 substituents selected from the group consisting of halogen, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.7 -C.sub.11 aralkyl, C.sub.6 -C.sub.10 aryl, C.sub.1 -C.sub.6 alkoxy and styrene polymer substituents.
摘要:
An optically active .beta.-aminoalkoxyborane complex of the formula (I): ##STR1## wherein R.sup.1 is C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.7 -C.sub.11 aralkyl or C.sub.6 -C.sub.10 aryl, R.sup.2 is hydrogen, C.sub.1 -C.sub.8 alkyl, C.sub.3 -C.sub.7 cycloalkyl or C.sub.7 -C.sub.11 aralkyl, or R.sup.1 and R.sup.2 together form (CH.sub.2).sub.n wherein n is 3 or 4, and Ar is naphthyl, anthryl or phenanthryl, which may be substituted by from 1 to 3 substituents selected from the group consisting of halogen, nitro, C.sub.1 -C.sub.6 alkyl, C.sub.3 -C.sub.7 cycloalkyl, C.sub.2 -C.sub.6 alkenyl, C.sub.2 -C.sub.6 alkynyl, C.sub.7 -C.sub.11 aralkyl, C.sub.6 -C.sub.10 aryl, C.sub.1 -C.sub.6 alkoxy and styrene polymer substituents.
摘要:
2-Phenylpropoionic acid ester of Formula (I): ##STR1## wherein R represents p-nitrophenyl group, .beta.-naphthyl group or 2-(.beta.-naphthyl)ethyl group.Optical resolution of the above is carried out by preferential crystallization by seeding either one of the optical isomers into a super-saturated solution of a racemic modification thereof or a mixture of the optical isomers thereof. The efficiency of the optical resolution can be increased by optional addition of a recemizing agent comprising a strongly basic amine or an alcholate.
摘要:
A process for preparing d-.alpha.-(6-methoxy-2-naphthyl)propionic acid, which comprises hydrolyzing an ester of d-.alpha.-(6-methoxy-2-naphthyl)propionic acid in an aqueous solution containing a basic catalyst.
摘要:
Disclosed is a process for preparing an optical active alkyl ester of .alpha.-(6-methoxynaphth-2-yl)propionic acid from the racemic modification thereof or from a mixture of the optical isomers thereof by preferential crystallization. The efficiency of the optical resolution can be increased by adding a base which facilitates the racemization. The process comprises dissolving the racemic modification or the optical isomers in an organic solvent such as methanol, ethanol, etc., with or without a base such as sodium methoxide, sodium ethoxide, etc., and seeding seed crystals of one of the optical isomers to effect crystallization for optical resolution.