专利名称：Synthesis of methylphenidate and analogs
thereof
发明人：Joseph P. Haar, Jr.,Carl J. Schaefer,Charles S.
Kuivila
申请号：US12652894申请日：20100106公开号：US08283472B2公开日：20121009
摘要：A synthetic process for the preparation of amino acid esters such asmethylphenidate and analogs thereof is disclosed. The process involves reacting anamino acid such as α-phenyl-α-(2-piperidinyl)acetic acid or an analog thereof with analcohol such as methanol in the presence of an acid and a water sequestrant such astrimethyl orthoacetate. In some embodiments, the water sequestrant is added to thereaction mixture after an initial period of esterification and then the reaction is allowed tocontinue. The α-phenyl-α-(2-piperidinyl)acetic acid methyl ester or analog thereof is thenisolated from the reaction mixture. In one variation of the process, the supernatant liquidmay be recycled in subsequent runs to increase yield and product purity.
申请人：Joseph P. Haar, Jr.,Carl J. Schaefer,Charles S. Kuivila
地址：Edwardsville IL US,Crestwood MO US,St. Louis MO US
国籍：US,US,US
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