Abstract:
An optically active amino acid derivative is produced by N-protecting an optically active 3-haloalanine derivative followed by cyclization, or cyclizing this derivative followed by N-protection to thereby give an optically active N-protected-aziridine-2-carboxylic acid derivative which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent, or by N-protecting an optically active 3-haloalanine derivative to thereby give N-protected-aziridine-2-carboxylic acid which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent. According to this process, natural and unnatural optically active amino acids can be produced from inexpensive materials by using simple procedures.
Abstract:
An optically active amino acid derivative is produced by N-protecting an optically active 3-haloalanine derivative followed by cyclization, or cyclizing this derivative followed by N-protection to thereby give an optically active N-protected-aziridine-2-carboxylic acid derivative which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent, or by N-protecting an optically active 3-haloalanine derivative to thereby give N-protected-aziridine-2-carboxylic acid which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent. According to this process, natural and unnatural optically active amino acids can be produced from inexpensive materials by using simple procedures.
Abstract:
La presente invención aborda el problema de proporcionar un parche con una adhesividad y fuerza cohesiva prácticas para uso medicinal, que proporcione un efecto anestésico inmediato. Se proporciona un parche formado por una capa adhesiva que contiene una mezcla de lidocaína con otro anestésico local en una cantidad de entre el 5 % en peso y el 20 % en peso. La capa adhesiva contiene al menos un adhesivo a base de caucho y parafina líquida, y el contenido de un agente de pegajosidad en la capa adhesiva no supera el 10 % en peso. (Traducción automática con Google Translate, sin valor legal)
Abstract:
An optically active amino acid derivative is produced by N-protecting an optically active 3-haloalanine derivative followed by cyclization, or cyclizing this derivative followed by N-protection to thereby give an optically active N-protected-aziridine-2-carboxylic acid derivative which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent, or by N-protecting an optically active 3-haloalanine derivative to thereby give N-protected-aziridine-2-carboxylic acid which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent. According to this process, natural and unnatural optically active amino acids can be produced from inexpensive materials by using simple procedures.
Abstract:
An optically active amino acid derivative is prepared either by subjecting a n 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 protecte d 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; R1 and R2 are each hydrogen or the like; * represents an asymmetric carbon atom; an d P1 is 2- and/ or 4- nitrated benzenesulfonyl.
Abstract:
An optically active amino acid derivative is produced by N-protecting an optically active 3-haloalanine derivative followed by cyclization, or cyclizing this derivative followed by N-protection to thereby give an optically active N-protected-aziridine-2-carboxylic acid derivative which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent, or by N-protecting an optically active 3-haloalanine derivative to thereby give N-protected-aziridine-2-carboxylic acid which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent. According to this process, natural and unnatural optically active amino acids can be produced from inexpensive materials by using simple procedures.
Abstract:
An optically active amino acid derivative is produced by N-protecting an optically active 3-haloalanine derivative followed by cyclization, or cyclizing this derivative followed by N-protection to thereby give an optically active N-protected-aziridine-2-carboxylic acid derivative which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent, or by N-protecting an optically active 3-haloalanine derivative to thereby give N-protected-aziridine-2-carboxylic acid which is protected by a benzenesulfonyl group substituted by nitro at the 2- and/or 4-positions and then treating this product with an organic metal reagent. According to this process, natural and unnatural optically active amino acids can be produced from inexpensive materials by using simple procedures.
Abstract:
This invention to provide a process for producing an optically active threo-phenylnorstatin derivative which does not require a toxic cyanating agent or a costly reagent, or a complicated procedure, and can be practiced on a commercial scale. This invention is directed to a process for producing a .beta.-amino-.alpha.-hydroxy acid derivative which comprises treating either a .gamma.-amino- .beta.-keto sulfoxide derivative with a halogenating agent to produce a .gamma.-amino-.alpha.-halo-.beta.-keto sulfoxide derivative, treating the same with an acid and an alcohol to produce a .beta. -amino- .alpha. -keto ester derivative or .beta.-amino- .alpha.-keto acid derivative, and followed by reducing.
Abstract:
PROBLEM TO BE SOLVED: To provide a method of selectively and efficiently removing the substituted carbamoyl group from the 2'-hydroxy group in a ribonucleoside derivative and/or an oligonucleic acid derivative including this ribonucleoside derivative as a constituting unit. SOLUTION: The method for efficiently producing a high purity oligonucleic acid comprises reacting a ribonucleoside derivative having a carbamoyl protective group for the 2'-hydroxy group and/or an oligonucleic acid derivative including this ribonucleoside derivative as a constituting unit with R 4 NF and removing the carbamoyl protective group from the 2'-hydroxy group. COPYRIGHT: (C)2011,JPO&INPIT