Gal J
J Pharm Sci. 1977 Feb;66(2):169-72. doi: 10.1002/jps.2600660209.
Amphetamine and eight related compounds were reacted with the chiral acylating reagent (-)-alpha-methoxy-alpha-(trifluoromethyl)phenylacetyl chloride to obtain, in each case, two diastereomeric amide derivatives. GLC conditions were found for the separation of the diastereomers in seven of the nine cases studied. This procedure may be suitable for the resolution of amino acid enantiomers via the amide derivatives of the methyl esters. Secondary amines were not derivatized under the reaction conditions used. A correlation between absolute configuration and elution order of the diastereomeric amides was observed for five compounds. The chiral acylating reagent was used in the determination of the enantiomeric composition of 2,5-dimethoxy-4-methylamphetamine excreted in rat urine after intraperitoneal drug administration. The chiral acylating reagent is suitable for the determination of the optical composition of compounds extracted from biological fluids.
将苯丙胺及八种相关化合物与手性酰化试剂（-）-α-甲氧基-α-（三氟甲基）苯乙酰氯反应，分别得到两种非对映体酰胺衍生物。在所研究的九个案例中的七个案例中，发现了用于分离非对映体的气相色谱条件。该方法可能适用于通过甲酯的酰胺衍生物拆分氨基酸对映体。在所用反应条件下，仲胺未被衍生化。观察到五种化合物的非对映体酰胺的绝对构型与洗脱顺序之间存在相关性。该手性酰化试剂用于测定腹腔注射药物后大鼠尿液中排泄的2,5-二甲氧基-4-甲基苯丙胺的对映体组成。该手性酰化试剂适用于测定从生物流体中提取的化合物的光学组成。
