Abstract:
A method for crystallizing the maleic acid salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-L-proline (Enalapril) from an aqueous liquid with ease in good yield, which comprises mixing an aqueous liquid containing N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-L-proline, maleic acid and a base and having a pH of 4 or more with an acid in an amount of the acid sufficient to convert the base to a neutral salt, to thereby crystallize N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-L-proline in the form of a maleic acid salt.
Abstract:
A method for crystallizing the maleic acid salt of N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-L-proline (Enalapril) from an aqueous liquid with ease in good yield, which comprises mixing an aqueous liquid containing N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-L-proline, maleic acid and a base and having a pH of 4 or more with an acid in an amount of the acid sufficient to convert the base to a neutral salt, to thereby crystallize N-(1(S)-ethoxycarbonyl-3-phenylpropyl)-L-alanyl-L-proline in the form of a maleic acid salt.
Abstract:
The present invention provides a process for reducing carbonyl compounds to hydroxy compounds, in particular stereoselectively reducing .alpha. -aminohaloketone derivatives, under mild conditions in an easy and simple manner, which comprises reacting a carbonyl compound of the general formula (1) with an organoaluminum compound of the general formual (4) to provide the corresponding alcohol compound of the general formula (5). (see fig. I) (see fig. II) (see fig. III)
Abstract:
PROBLEM TO BE SOLVED: To provide a method for producing a β-amino-α-hydroxy acid derivative by a process regarded to be efficiently and industrially usable. SOLUTION: The method for producing a β-amino-α-hydroxy acid derivative represented by general formula (2) comprises hydrolyzing an α-amino-α',α'-dihaloketone derivative represented by general formula (1) in the presence of a base and then protecting or non-protecting the amino group. COPYRIGHT: (C)2006,JPO&NCIPI
Abstract:
An optically active amino acid derivative is prepared either by subjecting an optically active 3-haloalanine derivative (1) to N-protection followed by cyclization or cyclization followed by N-protection to prepare an optically active aziridinecarboxylic acid derivative (3) whose imino group is protected with 2- and/or 4-nitrated benzenesulfonyl and treating this derivative (3) with an organometallic reagent or by subjecting an optically active 3-haloalanine derivative to N-protection to obtain an optically active 3-haloalanine derivative (4) whose amino group is protected with 2- and/or 4-nitrated benzenesulfonyl and treating this derivative (4) with an organometallic reagent. According to such processes, natural and nonnatural optically active amino acids can be prepared from inexpensive raw materials through simple and easy operation. In said derivatives, X is halogen; R?1 and R2¿ are each hydrogen or the like; * represents an asymmetric carbon atom; and P1 is 2- and/ or 4- nitrated benzenesulfonyl.
Abstract:
The present invention provides a process for reducing carbonyl compounds to hydroxy compounds, in particular stereoselectively reducing alpha -aminohaloketone derivatives, under mild conditions in an easy and simple manner, which comprises reacting a carbonyl compound of the general formula (1) with an organoaluminum compound of the general formual (4) to provide the corresponding alcohol compound of the general formula (5).
Abstract:
A process for preparing β-amino-α-hydroxy acid derivatives in an efficient and commercially useable manner. The process is characterized by hydrolyzing an α-amino-α',α'-dihaloketone derivative represented by general formula (1) in the presence of a base, optionally followed by the protection of the amino group, to prepare a β-amino-α-hydroxy acid derivative represented by general formula (2).
Abstract:
A method for producing a composition containing fucoxanthin includes a first step of adding a water-soluble solvent containing 0 to 80% by weight of water to seaweed to obtain a seaweed component extract, and then adding water and/or a water-soluble solvent to the seaweed component extract in such a manner that the concentration of the water-soluble solvent is 20 to 45% by weight and also adding a diluent thereto to obtain a diluent-containing extract, and a second step of stirring the diluent-containing extract, and then collecting a substance aggregating into the diluent-containing extract as a composition containing fucoxanthin by separation.
Abstract:
A high quality N-alcoxycarbonyl-tert leucine can be efficiently and stably produced with an easy procedure by reacting tert-leucine with an N-alcoxycarbonylating agent in the presence of water, wherein the use amount of the N-alcoxycarbonylating agent is not less than 0.90 times by mole and not more than 1.00 times by mole relative to the tert-leucine, with maintaining the pH of the reaction mixture in the range of not less than 9 and not more than 13 using a basic agent. In addition, an N-alcoxycarbonyl-tert-leucine can be efficiently extracted from the basic aqueous solution thereof under a mild condition using a water-immiscible solvent by mixing a hydroxide. Furthermore, the two crystal forms of N-butoxycarbonyl-tert-leucine can be controlled by adjusting the water amount in crystallization step, and the compound can be stably produced in an industrial production.
Abstract:
In the present invention, an N-protected amino acid is obtained by producing an amino acid using a biocatalyst such as a microorganism and enzyme; acidizing the reaction mixture containing the amino acid to adjust pH to not more than 4, without isolating the amino acid; and then protecting the amino group under a basic condition. As a result, a high-quality N-protected amino acid can be quantitatively and efficiently produced using a quantitative or slightly excessive protecting agent, even when the amino acid produced using a biocatalyst is directly protected without isolating the amino acid.