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1.发明授权Method of preparing .alpha.-L-aspartyl-L-phenylalanine methyl ester and its hydrochloride 失效制备α-L-天冬氨酰-L-苯丙氨酸甲酯及其盐酸盐的方法
公开(公告)号：US4606854A
公开(公告)日：1986-08-19
申请号：US611531
申请日：1984-05-17
CPC分类号： C07K5/0613
摘要： A method for preparing .alpha.-L-aspartyl-L-phenylalanine methyl ester and its hydrochloride which comprises dissolving .alpha.-L-aspartyl-L-phenylalanine dimethyl ester in a mixture of 0-10% (v/v) methanol, 8-55% (v/v) of concentrated hydrochloric acid, and water (remainder) to a concentration of 0.01 mol/dl to 0.30 mol/dl; holding the resulting solution at one or more temperatures between 0.degree. and 60.degree. C. for a time sufficient for crystals of .alpha.-L-aspartyl-L-phenylalanine methyl ester hydrochloride to precipitate out, and isolating the crystals. The hydrochloride may then be treated with alkali to yield .alpha.-L-aspartyl-L-phenylalanine methyl ester.
摘要翻译： 制备α-L-天冬氨酰-L-苯丙氨酸甲酯及其盐酸盐的方法，其包括将α-L-天冬氨酰基-L-苯丙氨酸二甲酯溶解在0-10％（v / v）甲醇，8-55 ％（v / v）浓盐酸和水（剩余物）至0.01mol / dl至0.30mol / dl的浓度; 将所得溶液保持在0℃至60℃之间的一个或多个温度下，足以使α-L-天冬氨酰基-L-苯丙氨酸甲酯盐酸盐的晶体沉淀出来，并分离晶体。 然后用碱处理盐酸盐，得到α-L-天冬氨酰基-L-苯丙氨酸甲酯。
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公开(公告)号：US4618695A
公开(公告)日：1986-10-21
申请号：US611548
申请日：1984-05-17
IPC分类号： C07K5/075 , C07C101/02
CPC分类号： C07K5/0613
摘要： A method of preparing .alpha.-L-phenylalanine methyl ester and its hydrochloride, which comprises dissolving .alpha.-L-aspartyl-L-phenylalanine .beta.-methyl ester in a methanol/hydrochloric acid mixture solvent which contains, when hydrochloric acid is expressed in terms of concentrated hydrochloric acid and water, 0 to 20% by volume of methanol, 8 to 55% by volume of concentrated hydrochloric acid and water (balance) in a concentration from 0.01 mol/dl to 0.3 mol/dl; holding the solution at 0.degree. to 60.degree. C. to effect intramolecular ester exchange reaction and crystallize out the formed .alpha.-L-aspartyl-L-phenylalanine methyl ester as its hydrochloride; isolating the hydrochloride; and obtaining, when required, the free ester by neutralization with an alkali, is disclosed.
摘要翻译： 一种制备α-L-苯丙氨酸甲酯及其盐酸盐的方法，其包括将α--L-天冬氨酰基-L-苯丙氨酸β-甲酯溶于甲醇/盐酸混合物溶剂中，所述溶剂含有当盐酸以 浓盐酸和水，0至20体积％甲醇，8至55体积％浓盐酸和水（余量），浓度为0.01mol / dl至0.3mol / dl; 将溶液保持在0〜60℃，进行分子内酯交换反应，结晶形成的α-L-天冬氨酰-L-苯丙氨酸甲酯为盐酸盐; 分离盐酸盐; 并且当需要时通过用碱中和获得游离酯。
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3.发明授权Process for producing .alpha.-L-aspartyl-L-phenylalanine methyl ester or its hydrohalide 失效制备α-L-天冬氨酰-L-苯丙氨酸甲酯或其氢卤酸盐的方法
公开(公告)号：US4634790A
公开(公告)日：1987-01-06
申请号：US700034
申请日：1985-02-11
IPC分类号： C07K1/12 , C07K5/075 , C07C101/32 , C07K5/06
CPC分类号： C07K5/0613
摘要： A process for producing .alpha.-L-aspartyl-L-phenylalanine methyl ester or its hydrohalide, which comprises subjecting 3-benzyl-6-carboxymethyl-2,5-diketopiperazine to partial hydrolysis with a strong acid in a solvent mixture of methanol and water.
摘要翻译： 一种生产α-L-天冬氨酰-L-苯丙氨酸甲酯或其氢卤酸盐的方法，其包括在甲醇和水的溶剂混合物中，用强酸将3-苄基-6-羧甲基-2,5-二酮哌嗪部分水解 。
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