CAS: 14976-57-9; (R)-2-(2-((R)-1-(4-Chlorophenyl)-1-Phenylethoxy)Ethyl)-1-Methylpyrrolidine Fumarate

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CAS号67004-64-2 1-甲基-2-吡咯烷乙醇 | CAS号59767-24-7 1-(4-氯苯基)-1-苯基乙醇 | CAS号134-85-0 4-氯二苯甲酮

N-甲基-2-(2-羟乙基)吡咯烷置于氯化亚砜,Sodium Amide,Sodium Hydroxide体系中,用 二氯甲烷,水,甲苯 用作溶剂,化学反应 4.0H,反应生成富马酸氯马斯汀
参考文献:一种富马酸氯马斯汀的制备方法
标题:一种富马酸氯马斯汀的制备方法
摘要:本发明涉及一种富马酸氯马斯汀的制备方法,所述方法,包括以下步骤:步骤1:以n‑甲基‑2‑(2‑羟乙基)吡咯烷为起始原料,对羟基进行氯化取代,制备得到n‑甲基‑2‑(2‑氯乙基)吡咯烷;步骤2:以n‑甲基‑2‑(2‑氯乙基)吡咯烷和1‑(4‑氯苯基)‑1‑苯基)乙醇为原料,在氨基钠的作用下反应得到消旋的氯马斯汀,再加入琥珀酸,制备得到消旋的氯马斯汀琥珀酸盐;步骤3:以消旋的氯马斯汀琥珀酸盐为原料,在丙酮和水中用l‑(+)‑酒石酸进行拆分,最后加入富马酸成盐得到富马酸氯马斯汀粗品;步骤4:富马酸氯马斯汀粗品,用丙酮水溶液进行重结晶,得到富马酸氯马斯汀纯品.

专利信息

专利号:US-2025206743-A1
优先权日:2022-03-25
标 题:Tyk2 inhibitor synthesis and intermediates thereof
发明人：MASSE CRAIG E; PHADKE AVINASH S; LAWSON JON P; LEVY STUART; YANG XIAOWEI; WU GUISHENG; FAN SHUFENG
权利人:TAKEDA PHARMACEUTICALS CO
摘要:Described herein are methods of synthesis of a tyrosine-protein kinase 2 (TYK2) inhibitor and to intermediate compounds of the synthesis and methods of making the intermediates. Also provided are pharmaceutically acceptable compositions including compounds prepared by the synthetic method and methods of treating disorders using the same.

专利号:US-12295961-B2
优先权日:2009-12-31
标 题:Modulation of solubility, stability, absorption, metabolism, and pharmacokinetic profile of lipophilic drugs by sterols
发明人：DHINGRA OM
权利人:MARIUS PHARMACEUTICALS INC
摘要:A formulation for drug delivery, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of a lipophilic therapeutic agent by formulation with sterols and/or sterol esters, resulting in higher bioavailability of a therapeutic agent administered to a subject in need of such therapeutic agent. The formulation contains a therapeutic agent and a sterol or sterol ester, and can, optionally, further contain a solubilizer and/or an enhancing agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

专利号:US-11617758-B2
优先权日:2009-12-31
标 题 :Emulsion formulations
发明人：DHINGRA OM; BERNSTEIN JAMES S
权利人:MARIUS PHARMACEUTICALS LLC
摘要:A SEDDS or SMEDDS or SNEDDS formulation for drug delivery of a lipophilic therapeutic agent, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of the therapeutic agent by formulation with a lipophilic surfactant, a hydrophilic surfactant, one or more solubilizers and, optionally, digestible oils, resulting in higher bioavailability of the therapeutic agent administered to a subject in need of such therapeutic agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

专利号:US-2013303495-A1
优先权日:2009-12-31
标题:Emulsion formulations
发明人：DHINGRA OM; BERNSTEIN JAMES S
权利人:SOV THERAPEUTICS; DIFFERENTIAL DRUG DEV ASSOCIATES LLC
摘要:A SEDDS or SMEDDS or SNEDDS formulation for drug delivery of a lipophilic therapeutic agent, providing enhanced modulation of solubility, stability, absorption, metabolism, and/or pharmacokinetic profile of the therapeutic agent by formulation with a lipophilic surfactant, a hydrophilic surfactant, one or more solubilizers and, optionally, digestible oils, resulting in higher bioavailability of the therapeutic agent administered to a subject in need of such therapeutic agent. Also described are pharmaceutical compositions containing the formulations and methods of making and methods of using the formulations and pharmaceutical compositions. Formulations of the disclosure can be constituted to minimize the synthesis of dihydrotestosterone when the therapeutic agent includes testosterone or testosterone esters.

专利号:CN-113087691-B
优先权日:2021-03-26
标题:A method for the synthesis of chiral aryl tertiary alcohols and benzopyrans based on a kinetic resolution strategy

专利号:EP-1930323-A1
优先权日:2004-03-11
标 题:Biphenyl compounds useful in the synthesis of muscarinic receptor antagonists