3-(3-(三氟甲基)苯基)Prop-2-Yn-1-醇置于5% Pd(II)/c(Eggshell) 氢气,Phosphorus Pentoxide,二甲基亚砜体系中,用 甲醇,二氯甲烷 用作溶剂,20.0 °C,101.33 Kpa 条件下,反应 72.0H,反应生成3-(3-三氟甲基苯基)丙醛 参考文献:A Process For The Preparation Of Cinacalcet And Intermediates Thereof 标题:A Process For The Preparation Of Cinacalcet And Intermediates Thereof
专利号:US-8614354-B2 优先权日:2008-06-18 标题 :Process for the synthesis of cinacalcet hydrochloride 发明人:FERRARI MASSIMO; GHEZZI MARCELLO; BONALDI MATTEO 权利人:FERRARI MASSIMO; GHEZZI MARCELLO; BONALDI MATTEO; ERREGIERRE SPA 摘要:There is described a process for the preparation of cinacalcet hydrochloride (I) which includes the steps of: a) reacting (R)-(+)-1-(1-naphthyl)ethylamine (II) with 3-[3-(trifluoromethyl)phenyl]propenaldehyde (III) to afford the non isolated intermediate (R)—N-[3-[3-(trifluoromethyl)phenyl]-2-propenylimino-N-[1-(1-naphthyl)ethylamine (IV); b) reducing the non isolated intermediate (R)—N-[3-[3-(trifluoromethyl)phenyl]-2-propenylimino-N-[-1-(1-naphthyl)ethylamine (IV) with a sequential addition of:—a solution of sodium borohydride, methanol and a base,—oxalic acid and—a base to obtain (R)—N-[3-[3-(tifluoromethyl)phenyl]-2-propenyl]-1-(1-naphthyl)ethylamine (V) by passing through the precipitation of the oxalate salt of compound (V) after the addition of oxalic acid; c) hydrogenating (R)—N-[3-[3-(trifluoromethyl)phenyl]-2-propenyl]-1-(1-naphthyl)ethylamine (V) thus obtaining (R)—N-(3-(3-(trifluoromethyl)phenyl]propyl]-1-(1-naphthyl)ethylamine cinacalcet base (VI), which is retaken in ethyl acetate; and d) treating the solution of cinacalcet base (VI) in ethyl acetate with hydrochloric acid to afford cinacalcet hydrochloride (I).
专利号:WO-2025099741-A1 优先权日:2023-11-07 标题:Process for the preparation of nitrosamine free cinacalcet and salts thereof 发明人:BIRARI DILIP RAMDAS; SHINDE GORAKSHANATH BALASAHEB; TELDHUNE Ashish Pramod 权利人:MEGAFINE PHARMA P LTD; BIRARI DILIP RAMDAS; SHINDE GORAKSHANATH BALASAHEB; TELDHUNE Ashish Pramod 摘要:The present invention relates to a process for preparation of nitrosamine free Cinacalcet (1) and salts thereof. Wherein, Cinacalcet (1) and its salts is substantially free of nitrosamine impurities by using of an antioxidant in the process for synthesis of Cinacalcet (1) and its pharmaceutically acceptable salts.
专利号:US-2010267988-A1 优先权日:2006-06-08 标 题:Processes for preparing intermediate compounds useful for the preparation of cinacalcet 发明人:SZEKERES TIBOR; REPASI JOZSEF; SZABO ANDRAS; MANGION BERNARDINO 权利人:MEDICHEM SA 摘要:The invention relates, in general, to an improved process for preparing compounds (e.g., 3-(3-trifluoromethylphenyl)propanal (Compound III, below)), which are key intermediates for the synthesis of cinacalcet, its salts and/or solvates thereof, as well as the use of such compounds prepared by such process for the preparation of cinacalcet and/or its salts or solvates.
专利号:EP-1990333-A1 优先权日:2007-05-11 标题 :Process for the preparation of cinacalcet hydrochloride 权利人:SANDOZ AG 摘要:The present invention relates to a process for the preparation of cinacalcet hydrochloride which is industrially feasible and commercially viable. The synthesis of cinacalcet hydrochloride is carried out by the condensation of 3-trifluromethylphenyl propionic acid with R-(+)-1-(lnaphthyl)ethylamine.
专利号:WO-2015071831-A1 优先权日:2013-11-18 标 题 :An improved process for minimising the formation of dehalogenated byproducts 发明人:KADAM SHASHIKANT; ARADDY RAJSHEKAR; KONDRAGUNTA VENKATESWARA RAO; HULAVALE YOGESH; SOMISETTI NARENDER RAO; CHENNAMSETTY SUNEEL MANOHAR BABU; HARIHARAN SIVARAMAKRISHNAN 权利人:PIRAMAL ENTPR LTD 摘要:The present invention provides an improved process for preparation of organic compounds represented by Formula-Z; wherein effectively minimising the formation of dehalogenated by-products is achieved. In the process, the reduction is carried out using suitable reducing agent; more preferably Lithium Aluminium Hydride (LAH) in a solvent system, wherein at least one of the solvent is selected from halogenated solvents, which acts as co-solvent. The process of the present invention is useful for minimising of the formation of dehalogenated by-products during synthesis of various active pharmaceutical ingredients such as Paroxetine Hydrochloride, Cinacalcet, Eletriptan and Asenapine.
专利号:US-7361789-B1 优先权日:2004-07-28 标 题 :Dihydronaphthalene compounds, compositions, uses thereof, and methods for synthesis 发明人:YAN QI; ORIHUELA CARLOS; SHEN BO; CHEN YING; WANG XIN; NG JOHN; JI RUIZHI; ZHOU PENGZU 权利人:AMGEN INC 摘要:The present invention relates to novel dihydronaphthalene compounds, compositions, methods for using the same, and processes for preparing the same. The present invention also relates to novel total synthesis approaches for preparing these compounds. In addition, the present invention relates to methods of producing quantities of isomers of these compounds and separating and purifying them using chiral separation techniques. The present invention also relates to methods of producing quantities of a single isometric compound without the need for chiral separation techniques.