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    • 3. 发明申请
    • Synthesis of Methylphenidate and Analogs Thereof
    • 哌甲酯及其类似物的合成
    • US20100179327A1
    • 2010-07-15
    • US12652894
    • 2010-01-06
    • Joseph P. Haar, JR.Carl J. SchaeferCharles S. Kuivila
    • Joseph P. Haar, JR.Carl J. SchaeferCharles S. Kuivila
    • C07D211/22
    • C07D211/60
    • A synthetic process for the preparation of amino acid esters such as methylphenidate and analogs thereof is disclosed. The process involves reacting an amino acid such as α-phenyl-α-(2-piperidinyl)acetic acid or an analog thereof with an alcohol such as methanol in the presence of an acid and a water sequestrant such as trimethyl orthoacetate. In some embodiments, the water sequestrant is added to the reaction mixture after an initial period of esterification and then the reaction is allowed to continue. The α-phenyl-α-(2-piperidinyl)acetic acid methyl ester or analog thereof is then isolated from the reaction mixture. In one variation of the process, the supernatant liquid may be recycled in subsequent runs to increase yield and product purity.
    • 公开了用于制备氨基酸酯如哌甲酯及其类似物的合成方法。 该方法包括在酸和水多价螯合剂如原乙酸三甲酯存在下使氨基酸如α-苯基-α-(2-哌啶基)乙酸或其类似物与醇如甲醇反应。 在一些实施方案中,在酯化的初始阶段之后,将水螯合剂加入到反应混合物中,然后使反应继续进行。 然后从反应混合物中分离α-苯基-α-(2-哌啶基)乙酸甲酯或其类似物。 在该方法的一个变化方案中,上清液可以在随后的运行中再循环以提高产率和产物纯度。
    • 7. 发明授权
    • Synthesis of methylphenidate and analogs thereof
    • 哌甲酯及其类似物的合成
    • US08283472B2
    • 2012-10-09
    • US12652894
    • 2010-01-06
    • Joseph P. Haar, Jr.Carl J. SchaeferCharles S. Kuivila
    • Joseph P. Haar, Jr.Carl J. SchaeferCharles S. Kuivila
    • C07D211/34
    • C07D211/60
    • A synthetic process for the preparation of amino acid esters such as methylphenidate and analogs thereof is disclosed. The process involves reacting an amino acid such as α-phenyl-α-(2-piperidinyl)acetic acid or an analog thereof with an alcohol such as methanol in the presence of an acid and a water sequestrant such as trimethyl orthoacetate. In some embodiments, the water sequestrant is added to the reaction mixture after an initial period of esterification and then the reaction is allowed to continue. The α-phenyl-α-(2-piperidinyl)acetic acid methyl ester or analog thereof is then isolated from the reaction mixture. In one variation of the process, the supernatant liquid may be recycled in subsequent runs to increase yield and product purity.
    • 公开了用于制备氨基酸酯如哌甲酯及其类似物的合成方法。 该方法包括在酸和水多价螯合剂如原乙酸三甲酯存在下使氨基酸如α-苯基-α-(2-哌啶基)乙酸或其类似物与醇如甲醇反应。 在一些实施方案中,在酯化的初始阶段之后,将水螯合剂加入到反应混合物中,然后使反应继续进行。 然后从反应混合物中分离α-苯基-α-(2-哌啶基)乙酸甲酯或其类似物。 在该方法的一个变化方案中,上清液可以在随后的运行中再循环以提高产率和产物纯度。