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    • 4. 发明申请
    • A PROCESS FOR PREPARATION OF ADAPALENE
    • 一种制备ADAPALENEN的方法
    • WO2007125542A3
    • 2007-12-27
    • PCT/IN2007000145
    • 2007-04-09
    • USV LTDTARUR RADHAKRISHNAN VENKATASUBBHISE NANDU BABANSATHE DHANANJAY GOVINDPATNEKAR SUBODH SHASHIKANTPATIL SACHIN SHIVAJI
    • TARUR RADHAKRISHNAN VENKATASUBBHISE NANDU BABANSATHE DHANANJAY GOVINDPATNEKAR SUBODH SHASHIKANTPATIL SACHIN SHIVAJI
    • A61K31/192A61P17/10C07C41/16C07C43/225C07C51/09C07C65/26C07C67/343
    • C07C67/343C07C41/16C07C51/09C07C51/412C07C2603/74C07C65/26C07C69/94C07C43/225
    • The present invention discloses a process for preparation of highly pure Adapalene, chemically designated as 6-[3-(l-adamantyl)-4-methoxy phenyl]-2-naphthoic acid (I) comprising: a) reacting 1-adamantanol with 4-bromophenol (II) in presence of sulphonic acid with or without the use of organic solvent to give 2-(l-adamantyl)-4- bromophenol (III); b) alkylating compound of formula(III) with dimethylsulphate in presence of base in organic solvent to obtain 2-(l-adamantyl)-4-bromoanisole (IV); c) C-C coupling the compound of formula (IV) with methyl-6-bromo-2- naphthoate using magnesium, purified zinc chloride and NiCl 2 -DPPE in THF at a temperature of 40-60°C tO obtain methyl ester of 6-[3-(l- adamantyl)-4-methoxy phenyl] -2-naphthoic acid (V); d) purifying crude methyl ester of 6-[3-(l-adamantyl)-4-methoxy phenyl]-2- naphthoic acid (V) using a mixture of organic solvent to obtain pure compound (V); e) hydrolyzing the compound (V) with a solution of alkali in organic solvent to obtain metal salt of 6-[3-(l-adamantyl)-4-methoxy phenyl] -2-naphthoic acid (VI); f) acidifying metal salt of adapalene (VI) using organic or inorganic acid to obtain crude adapalene (I) and g) recrystallizing the crude adapalene (I) using a mixture of organic solvents to obtain pure adapalene (I).
    • 本发明公开了一种制备高纯度阿达帕林的方法,化学名为6- [3-(1-金刚烷基)-4-甲氧基苯基] -2-萘甲酸(I),其包括:a)使1-金刚烷醇与4 (II)在有或没有使用有机溶剂的情况下在磺酸存在下反应,得到2-(1-金刚烷基)-4-溴酚(III); b)在碱的存在下,在有机溶剂中,用式(III)的化合物与硫酸二甲酯烷基化,得到2-(1-金刚烷基)-4-溴苯甲醚(Ⅳ); c)在40-60℃的温度下,使用镁,纯化氯化锌和NiCl 2 -DPPE在THF中将式(Ⅳ)化合物与6-溴-2-萘甲酸甲酯偶联, 得到6- [3-(1-金刚烷基)-4-甲氧基苯基] -2-萘甲酸(V)的甲酯。 d)使用有机溶剂的混合物纯化6- [3-(1-金刚烷基)-4-甲氧基苯基] -2-萘甲酸(V)的粗甲酯,得到纯的化合物(V); e)用碱在有机溶剂中的溶液水解化合物(V),得到6- [3-(1-金刚烷基)-4-甲氧基苯基] -2-萘甲酸(Ⅵ)的金属盐。 f)使用有机或无机酸酸化阿达帕林(VI)的金属盐,得到粗制阿达帕林(I),和g)使用有机溶剂的混合物重结晶粗制阿达帕林(I),得到纯的阿达帕林(I)。
    • 5. 发明申请
    • A PROCESS FOR THE PREPARATION OF 5-[4-[2-[N-METHYL-N-(2-PYRIDYL) AMINO] ETHOXY] PHENYL METHYL] THIAZOLIDINE-2, 4-DIONE MALEATE
    • 制备5- [4- [2- [N-甲基-N-(2-吡啶基)氨基]乙氧基]苯基甲基]噻唑烷-2,4-二酮缩醛的方法
    • WO2005073227B1
    • 2005-11-17
    • PCT/IN2004000271
    • 2004-08-31
    • USV LTD
    • TARUR VENKATASUBRAMANIAN RADHAKADAM SURESH MAHADEVGEDIYA LALJI KARSANPATNEKAR SUBODH SHASHIKANT
    • C07D417/12
    • C07D417/12
    • The present invention discloses a process for the preparation of 5-[4-[2-[N-methyl-N-(2-pyridyl) amino] ethoxy] phenyl methyl] thiazolidine-2,4-dione maleate (VI) comprising the steps of Coupling 2-[N-methyl-N-(2-pyridyl) amino] ethanol (I) and 4-fluorobenzaldehyde (II) in N, N-dimethylformamide, isolating the coupled product 4-[2-[N-methyl-N-(2-pyridyl) amino] ethoxy] benzaldehyde (III), converting said isolated benzaldehyde compound (III) to 5-[4-[2-[N-methyl-N-(2-pyridyl) amino] ethoxy] benzylidene] thiazolidine-2,4-dione (IV) and purifying the same, reducing 5-[4-[2-[N-methyl-N-(2-pyridyl) amino] ethoxy] benzylidene] thiazolidine-2,4-dione, by a novel reduction method for making 5-[4-[2-[N-methyl-N-(2-pyridyl)amino]ethoxy] phenyl methyl] thiazolidine-2,4-dione (V). This reduction method involves reacting the compound (IV) with a novel metal legand complex and a reducing agent, purifying the product (V) obtained by a new method reported in the present invention and converting the said thiazolidine-2,4-dione compound (V) into a pharmaceutically acceptable salt.
    • 本发明公开了一种制备5- [4- [2- [N-甲基-N-(2-吡啶基)氨基]乙氧基]苯基甲基]噻唑烷-2,4-二酮马来酸酯(VI)的方法, 在N,N-二甲基甲酰胺中偶联2- [N-甲基-N-(2-吡啶基)氨基]乙醇(I)和4-氟苯甲醛(II)的步骤,分离偶联产物4- [2- [N-甲基 -N-(2-吡啶基)氨基]乙氧基]苯甲醛(III),将所述分离的苯甲醛化合物(III)转化为5- [4- [2- [N-甲基-N-(2-吡啶基)氨基]乙氧基] 亚苄基]噻唑烷-2,4-二酮(IV),并纯化,得到5- [4- [2- [N-甲基-N-(2-吡啶基)氨基]乙氧基]亚苄基]噻唑烷-2,4-二酮 通过制备5- [4- [2- [N-甲基-N-(2-吡啶基)氨基]乙氧基]苯基甲基]噻唑烷-2,4-二酮(V)的新的还原方法。 该还原方法包括使化合物(IV)与新型金属配合物和还原剂反应,纯化通过本发明报道的新方法获得的产物(V),并将所述噻唑烷-2,4-二酮化合物 V)转化为药学上可接受的盐。