CAS: 19395-41-6; Ritalinic Acid

上下游产品

(+/-)-erythro/threo-2-phenyl-2-(piperidin-2-yl)acetamide 2-phenyl-2-(pyridin-2-yl)acetamide phenyl-pyridin-2-yl-acetonitrile 1-piperidin-1-yl-ethanoneMETHYLPHENIDATE dl-threo-methylphenidate methyl (R*)-2-phenyl-2-((S*)-piperidin-2-yl)acetate (1-pentafluoropropionyl-piperidin-2-yl)-phenyl-acetic acid methyl ester

苯基-(2-吡啶基)乙酰胺置于platinum On Activated Charcoal 盐酸,氢氧化钾,氢气体系中,用 溶剂黄146 用作溶剂,化学反应 16.0H,反应生成利太林酸
参考文献:潜在可卡因拮抗剂的合成和药理作用.2.芳环取代的哌醋甲酯类似物的结构-活性关系研究.
标题:潜在可卡因拮抗剂的合成和药理作用.2.芳环取代的哌醋甲酯类似物的结构-活性关系研究.
摘要:作为开发可阻断可卡因与多巴胺转运蛋白结合而又不吸收多巴胺的药物的计划的一部分,合成了一系列芳香环取代的哌醋甲酯衍生物,并测试了其对[3H] Win 35,428结合和[使用大鼠纹状体组织的3H]多巴胺摄取测定.通过将2-溴吡啶与衍生自各种取代的苯基乙腈的阴离子进行烷基化来完成合成.在大多数情况下,赤型化合物的效力明显低于相应的(+/-)-苏式-甲基-哌醋甲酯(tmp;利他林)衍生物.邻位取代的化合物的效力远低于相应的间位和/或对位取代的衍生物.对抗[3H] Win 35,428结合的最有效化合物,M-Bromo-Tmp,比母体化合物的效力高20倍,而对[3H]多巴胺摄取最有效的化合物m,P-Dichloro-Tmp则强32倍.具有m-或p-卤代取代基的threo衍生物比tmp更有力,而给电子的取代基引起的变化很小或失去的效力很小.除m,P-Dichloro-Tmp(nh为2.0)外,所有导
Doi:10.1021/jm950697C

专利信息

专利号:US-5733756-A
优先权日:1996-01-05
标 题:Lactams and processes for stereoselective enrichment of lactams, amides, and esters
发明人：ZEITLIN ANDREW L; STIRLING DAVID I
权利人:CELGENE CORP
摘要:Novel lactams and processes for the preparation of chiral compounds having utility as intermediates in the synthesis of compounds with Central Nervous System stimulant activity.

专利号:US-8283472-B2
优先权日:2009-01-09
标题:Synthesis of methylphenidate and analogs thereof
发明人：HAAR JR JOSEPH P; SCHAEFER CARL J; KUIVILA CHARLES S
权利人:HAAR JR JOSEPH P; SCHAEFER CARL J; KUIVILA CHARLES S; MALLINCKRODT LLC
摘要: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.

专利号:US-9475770-B2
优先权日:2010-12-17
标 题 :Low-temperature synthesis of methylphenidate hydrochloride
发明人：HUNTLEY C FREDERICK M; KATAISTO ERIK WAYNE; LA LUMIERE KNICHOLAUS DUDLEY; REISCH HELGE ALFRED
权利人:HUNTLEY C FREDERICK M; KATAISTO ERIK WAYNE; LA LUMIERE KNICHOLAUS DUDLEY; REISCH HELGE ALFRED; RHODES TECH
摘要:The present invention describes a process for the preparation of methylphenidate hydrochloride. The process involves the esterification of ritalinic acid and methanol in the presence of an acid catalyst at a low temperature. The process may optionally involve the addition of an orthoester.

专利号:US-9453037-B2
优先权日:2011-07-28
标 题 :Methylphenidate-prodrugs, processes of making and using the same
发明人：GUENTHER SVEN; CHI GUOCHEN; BERA BINDU; MICKLE TRAVIS; BERA SANJIB
权利人:KEMPHARM INC; KEMPHARM INC
摘要:The present technology is directed to prodrugs and compositions for the treatment of various diseases and/or disorders comprising methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof. In some embodiments, the conjugates further include at least one linker. The present technology also relates to the synthesis of methylphenidate, or methylphenidate derivatives, conjugated to at least one alcohol, amine, oxoacid, thiol, or derivatives thereof or combinations thereof.

专利号:US-6486355-B1
优先权日:2000-02-23
标 题:Application of chiral critical clusters to assymetric synthesis
发明人：FERRIERI RICHARD A
权利人:BROOKHAVEN SCIENCE ASS LLC
摘要:Disclosed is a composition, a method of making and a method of using critical clusters for asymmetric synthesis using substantially optically-pure chiral solvent molecules in a supercritical fluid. The solvent molecules are capable of forming a multipoint hydrogen bonded solvate as they encage at least one solute molecule. The encaged solute molecule is capable of reacting to form an optically active chiral center. In another aspect, there is disclosed a method of directing the position of bonding between a solute molecule and a ligand involving encaging the solute molecule and the ligand with polar solvent molecules in a supercritical fluid under conditions of temperature and pressure sufficient to change electric charge distribution in the solute molecule. In yet another aspect, disclosed is a method of making pharmaceutical compounds involving encaging a solute molecule, which is capable of forming a chiral center, and a ligand with polar solvent molecules in a supercritical fluid under conditions of temperature and pressure sufficient to change electric charge distribution of the solute molecule. The solute molecule and ligand are then reacted whereby the ligand bonds to the solute molecule forming a chiral center. Also disclosed is a method for racemic resolution using critical clusters involving encaging racemic mixtures of solute molecules with substantially optically-pure chiral solvent molecules in a supercritical fluid under conditions of temperature and pressure sufficient to form critical clusters. The solvent molecules are capable of multipoint hydrogen bonding with the solute molecules. The encaged solute molecules are then nonenzymatically reacted to enhance the optical purity of the solute molecules.

专利号:CA-2822016-C
优先权日:2010-12-17
标题:Low-temperature synthesis of methylphenidate hydrochloride