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Production manner of optical active aminophosphonic acid derivative and production manner and new phosphonate type chemical compound null general formula (ii)
Production manner of optical active aminophosphonic acid derivative and production manner and new phosphonate type chemical compound null general formula (ii)
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机译:光学活性氨基膦酸衍生物的生产方法及新型膦酸酯类化合物无效通式(ii)的生产方法
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摘要
PURPOSE: To produce an optically active α-aminophosphonic acid derivative useful as an antimicrobial gent, etc., by reacting an imine with a phosphonic acid ester in the presence of a specific catalyst for asymmetric synthesis and then deprotecting and hydrolyzing the produced phosphonate compound by contact with an acid or hydrogen. ;CONSTITUTION: An imine of formula I (R1 is trityl, benzyl or di-p-anisylmethyl; R2 is an alkyl, a cycloalkyl, an aryl or a hydrocarbon containing an aryl group) is reacted with a phosphonic acid ester of formula II (R3 is an alkyl, a cycloalkyl, an allyl, an aryl, etc.) in the presence of a catalyst for asymmetric synthesis of the formula La-X-binaphthol (X is an alkali metal) to synthesize a phosphonate-based compound of formula III or IV, which is then brought into contact with an acid or hydrogen to carry out the deprotection or hydrolysis. Thereby, the objective optically active α-aminophosphonic acid derivative of formula V or VI, partially containing a new compound and having antimicrobial activities is efficiently obtained in a large amount.;COPYRIGHT: (C)1996,JPO
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机译:用途:通过在不对称合成的特定催化剂存在下使亚胺与膦酸酯反应,然后脱保护并水解所生成的膦酸酯化合物,来制备可用作抗菌剂等的旋光性α-氨基膦酸衍生物。通过与酸或氢接触。 ;组成:式Ⅰ的亚胺(R 1 Sup>是三苯甲基,苄基或二对茴香基甲基; R 2 Sup>是烷基,环烷基,芳基或烃在不对称合成催化剂的存在下,使含有芳基的化合物与式Ⅱ的膦酸酯(R 3 Sup>为烷基,环烷基,烯丙基,芳基等)反应式La-X-联萘酚(X是碱金属)的式(I)合成基于膦酸酯的式III或IV的化合物,然后使其与酸或氢接触以进行脱保护或水解。从而,有效地大量大量地获得了部分含有新化合物并具有抗菌活性的目标式V或VI的光学活性α-氨基膦酸衍生物。COPYRIGHT:(C)1996,JPO
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