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    PROCESS FOR PREPARING HIGH PURITY URSODEOXYCHOLIC ACID
    1.
    发明申请
    PROCESS FOR PREPARING HIGH PURITY URSODEOXYCHOLIC ACID 审中-公开
    制备高纯度羟基氧化酸的方法

    公开(公告)号：WO2014020024A1

    公开(公告)日：2014-02-06

    申请号：PCT/EP2013/066002

    申请日：2013-07-30

    Applicant: ERREGIERRE S.P.A.

    Inventor： FERRARI, Massimo ,  ZINETTI, Fabrizio

    IPC: C07J75/00

    CPC classification number: C07J9/005 ,  C07J75/00

    Abstract: The present invention describes a process for the synthesis of ursodeoxycholic acid wherein the purification of the crude ursodeoxycholic acid (containing approximately 13-15% of chenodeoxycholic acid impurity) takes place first passing through a salification with imidazole and a subsequent purification via "methyl ester", which allows a finished product with an extremely low content of known "cheno and "litho" impurities to be obtained. The present invention also describes the recovery steps of cholic acid and 3α-hydroxy-7-ketocholanic acid from the mother liquors of process intermediates.

    Abstract translation: 本发明描述了一种合成熊去氧胆酸的方法，其中首先通过用咪唑进行成盐，然后通过“甲酯”纯化纯化粗脱氧胆酸（含有约13-15％的鹅脱氧胆酸杂质） ，其可以获得具有极低含量的已知“苯酚”和“光刻”杂质的成品，本发明还描述了从过程的母液中获得的胆酸和3α-羟基-7-酮基胆酸的回收步骤 中间体。

    PROCESS FOR CRYSTALLISING BUPROPION HYDROCHLORIDE
    2.
    发明申请
    PROCESS FOR CRYSTALLISING BUPROPION HYDROCHLORIDE 审中-公开
    结晶氯化氢溶液的方法

    公开(公告)号：WO2004089873A1

    公开(公告)日：2004-10-21

    申请号：PCT/EP2004/050495

    申请日：2004-04-09

    Applicant: ERREGIERRE S.P.A. ,  FERRARI, Massimo ,  DE LUCA, Florindo ,  LOMBARDI, Fiorella

    Inventor： FERRARI, Massimo ,  DE LUCA, Florindo ,  LOMBARDI, Fiorella

    IPC: C07C221/00

    CPC classification number: C07C221/00 ,  C07C225/16

    Abstract: Process for crystallising Bupropion hydrochloride comprising the following stages: a) Bupropion hydrochloride is dissolved in a mixture comprising methanol and a precipitating solvent for Bupropion hydrochloride; b) any insoluble residue is removed; c) the solution is distilled at atmospheric pressure until the precipitation reaction is triggered; d) the following are added: I) a precipitating solvent for Bupropion hydrochloride and II) hydrochloric acid until a pH ≤ 2 is obtained; e) the mass is cooled to a temperature less than 10° C, preferably between 0 and 3° C and the precipitate obtained is separated.

    Abstract translation: 用于结晶的盐酸安非他酮的方法，包括以下阶段：a）将盐酸安非他酮溶于包含甲醇和沉淀溶剂的混合物中，用于安非他酮盐酸盐; b）除去任何不溶性残留物; c）将溶液在大气压下蒸馏直至引发沉淀反应; d）加入以下物质：I）盐酸安非他酮的沉淀溶剂和II）盐酸，直至获得pH <= 2; e）将物质冷却至低于10℃，优选0至3℃的温度，并将所得沉淀物分离。

    A PROCESS FOR SYNTHESIS OF 1-(AMINOMETHYL)CYCLOHEXANE ACETIC ACID HYDROCHLORIDE
    4.
    发明申请
    A PROCESS FOR SYNTHESIS OF 1-(AMINOMETHYL)CYCLOHEXANE ACETIC ACID HYDROCHLORIDE 审中-公开
    合成1-（氨基甲基）环己烷醋酸氢氯酸盐的方法

    公开(公告)号：WO2004031126A2

    公开(公告)日：2004-04-15

    申请号：PCT/EP2003/010866

    申请日：2003-10-01

    Applicant: ERREGIERRE S.p.A. ,  FERRARI, Massimo ,  GHEZZI, Marcello ,  BELOTTI, Paolo

    Inventor： FERRARI, Massimo ,  GHEZZI, Marcello ,  BELOTTI, Paolo

    IPC: C07C229/00

    CPC classification number: C07C227/12 ,  C07C229/28

    Abstract: A process for synthesis of 1-(aminomethyl)cyclohexane acetic acid hydrochloride (Gabapentin hydrochloride) comprising: a) Reaction of a mixture of acetic anhydride/ammonium acetate with 1,1-cyclohexane­diacetic acid to yield 3,3-pentamethylene glutarimide; b) Treatment of 3,3-pentamethylene glutarimide with sodium hydroxide in an aqueous solution up to dissolution, dripping the solution thus obtained into a to sodium hydroxide/sodium hypochlorite mixture, which is also aqueous, followed by acidification with hydrochloric acid to yield gabapentine hydrochloride.

    Abstract translation: 合成1-（氨基甲基）环己烷乙酸盐酸盐（盐酸加巴喷丁）的方法，其包括：a）将乙酸酐/乙酸铵与1,1-环己烷＆shy;二乙酸的混合物与 得到3,3-戊二酰戊二酰亚胺; b）用氢氧化钠在水溶液中处理3,3-戊二酰戊二酰亚胺直至溶解，将由此获得的溶液滴加到也为含水的氢氧化钠/次氯酸钠混合物中，然后用盐酸酸化以产生加巴喷丁 盐酸盐。

    PROCESS FOR THE PRODUCTION OF DEFERASIROX
    6.
    发明申请
    PROCESS FOR THE PRODUCTION OF DEFERASIROX 审中-公开
    生产DEFERASIROX的方法

    公开(公告)号：WO2012131017A1

    公开(公告)日：2012-10-04

    申请号：PCT/EP2012/055753

    申请日：2012-03-30

    Applicant: ERREGIERRE S.P.A. ,  FERRARI, Massimo ,  GALLI, Matteo

    Inventor： FERRARI, Massimo ,  GALLI, Matteo

    IPC: C07D249/08

    CPC classification number: C07D249/08

    Abstract: A new process is described for the preparation of deferasirox, 4-[(3 Z ,5 E )-3,5-bis(6- oxo-1 -cyclohexa-2,4-dienylidene)-1,2,4-triazolidin-1 -yl]benzoic acid, having the following structural formula (I).

    Abstract translation: 描述了一种新的方法，用于制备去甲草酮，4 - [（3Z，5E）-3,5-双（6-氧代-1-环己基-2,4-二亚烯基）-1,2,4-三唑烷-1 - 基]苯甲酸，具有以下结构式（I）。

    A PROCESS FOR THE SYNTHESIS OF CINACALCET HYDROCHLORIDE
    7.
    发明申请
    A PROCESS FOR THE SYNTHESIS OF CINACALCET HYDROCHLORIDE 审中-公开
    CINACALCET HYDROCHLORIDE的合成方法

    公开(公告)号：WO2009153814A1

    公开(公告)日：2009-12-23

    申请号：PCT/IT2008/000404

    申请日：2008-06-18

    Applicant: ERREGIERRE S.p.A. ,  FERRARI, Massimo ,  GHEZZI, Marcello ,  BONALDI, Matteo

    Inventor： FERRARI, Massimo ,  GHEZZI, Marcello ,  BONALDI, Matteo

    IPC: C07C209/28 ,  C07C211/30

    CPC classification number: C07C209/28 ,  C07C211/30

    Abstract: 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 - naphthyi)ethy!amine (IV); b) reducing the non isolated intermediate (R)-N-[3-[3-(trifluoromethyl)phenyl]-2-propenylimine-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-(trifluoromethyl)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]propyij-i-(i -naphthyl)ethylamine cinacalcet base (Vl), 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).

    Abstract translation: 描述了制备西那卡塞盐酸盐（I）的方法，其包括以下步骤：a）使（R） - （+） - 1-（1-萘基）乙胺（II）与3- [3-（三氟甲基） ）苯基]丙醛（III），得到非分离的中间体（R）-N- [3- [3-（三氟甲基）苯基] -2-丙烯基亚氨基-N- [1-（1-萘基）乙基胺（IV ）; b）依次加入非离子中间体（R）-N- [3- [3-（三氟甲基）苯基] -2-丙烯基亚胺-N - [1-（1-萘基）乙胺（IV））， - 硼氢化钠，甲醇和碱的溶液 - 草酸和碱，得到（R）-N- [3- [3-（三氟甲基）苯基] -2-丙烯基] -1-（1-萘基 ）乙胺（V）通过在加入草酸后通过化合物（V）的草酸盐的沉淀; c）氢化（R）-N- [3- [3-（三氟甲基）苯基] -2-丙烯基] -1-（1-萘基）乙胺（V），由此得到（R）-N-（3-（3 - （三氟甲基）苯基]丙基] - （1-萘基）乙胺西那卡塞碱（VI），其在乙酸乙酯中再次;和d）用盐酸将西那卡赛碱（Vi）溶液在乙酸乙酯中处理，得到 盐酸西那卡塞（I）。

    PROCESS FOR PREPARING 2-METHOXYCARBONYLMETHYL-6,6-DIMETHYL-2- TETRAHYDROPYRAN CARBOXYLIC ACID
    9.
    发明申请
    PROCESS FOR PREPARING 2-METHOXYCARBONYLMETHYL-6,6-DIMETHYL-2- TETRAHYDROPYRAN CARBOXYLIC ACID 审中-公开
    制备2-甲氧基羰基甲基-6,6-二甲基-2-四氢吡喃羧酸的方法

    公开(公告)号：WO2007009953A1

    公开(公告)日：2007-01-25

    申请号：PCT/EP2006/064273

    申请日：2006-07-14

    Applicant: ERREGIERRE S.p.A. ,  STRAGEN PHARMA SA ,  FERRARI, Massimo ,  BELOTTI, Paolo

    Inventor： FERRARI, Massimo ,  BELOTTI, Paolo

    IPC: C07D309/08 ,  C07C211/35 ,  C07D491/20

    CPC classification number: C07C211/35 ,  C07D309/08

    Abstract: Process for preparing 2-methoxycarbonylmethyl-6,6-dimethyl-2-tetrahydropyran carboxylic acid (I) comprising: a) Reaction of 5-bromo-2-methyl-2-pentene (III) with magnesium and then diethyloxalate to obtain ethyl-2-oxo-6-methyl-5-heptenoate (IV); b) Reaction of ethyl-2-oxo-6-methyl-5-heptenoate (IV) with an alkali amide and methyl acetate to obtain ethyl-2- methoxycarbonylmethyl^-hydroxy-θ-methyl- 5-heptenoate (V); c) Reaction of ethyl-2- methoxycarbonylmethyl-2-hydroxy-6-methyl-5-heptenoate (V) with an alkali metal hydroxide to obtain the corresponding 2-carboxymethyl- 2-hydroxy-6-methyl-5-heptenoic acid (Vl); d) Cyclisation of 2-carboxymethyl-2-hydroxy-6-methyl-5-heptenoic acid (Vl) with formic acid to give 2-carboxymethyl-6,6-dimethyl-2-tetrahydropyrancarboxylic acid (VII); e) Monoesterification of 2-carboxymethyl-6,6-dimethyl-2- tetrahydropyrancarboxylic acid (VII) to 2-methoxycarbonylmethyl-6,6-dimethyl- 2-tetrahydropyran carboxylic acid (I), characterised in that in stage (e) the 2-methoxycarbonylmethyI-6,6-dimethyl-2- tetrahydropyran carboxylic acid (I) is purified by means of the formation of the corresponding salt with cyclohexylamine (IA).

    Abstract translation: 制备2-甲氧基羰基甲基-6,6-二甲基-2-四氢吡喃羧酸（I）的方法，包括：a）将5-溴-2-甲基-2-戊烯（III）与镁反应，然后用二乙基草酸酯反应，得到乙基 - 2-氧代-6-甲基-5-庚烯酸酯（IV）; b）乙基-2-氧代-6-甲基-5-庚烯酸乙酯（Ⅳ）与碱金属酰胺和乙酸甲酯反应得到乙基-2-甲氧基羰基甲基-4-羟基-α-甲基-5-庚烯酸甲酯（Ⅴ）; c）将乙基-2-甲氧基羰基甲基-2-羟基-6-甲基-5-庚烯酸乙酯（V）与碱金属氢氧化物反应，得到相应的2-羧甲基-2-羟基-6-甲基-5-庚烯酸（ VL）; d）用甲酸使2-羧甲基-2-羟基-6-甲基-5-庚烯酸（VI）环化，得到2-羧甲基-6,6-二甲基-2-四氢吡喃羧酸（VII）; e）将2-羧甲基-6,6-二甲基-2-四氢吡喃羧酸（VII）单酯化为2-甲氧基羰基甲基-6,6-二甲基-2-四氢吡喃羧酸（I），其特征在于在步骤（e）中， 通过与环己胺（IA）形成相应的盐来纯化2-甲氧基羰基甲基-6,6-二甲基-2-四氢吡喃羧酸（I）。

    PROCESS FOR PREPARING RALOXIFENE HYDROCHLORIDE
    10.
    发明申请
    PROCESS FOR PREPARING RALOXIFENE HYDROCHLORIDE 审中-公开
    制备雷洛芬芬氢氯化物的方法

    公开(公告)号：WO2005003116A1

    公开(公告)日：2005-01-13

    申请号：PCT/EP2004/051263

    申请日：2004-06-28

    Applicant: ERREGIERRE S.p.A. ,  FERRARI, Massimo ,  ZINETTI, Fabrizio ,  BELOTTI, Paolo

    Inventor： FERRARI, Massimo ,  ZINETTI, Fabrizio ,  BELOTTI, Paolo

    IPC: C07D333/56

    CPC classification number: C07D333/56

    Abstract: Process for preparing raloxifene hydrochloride with a purity greater than 98% and low aluminium content comprising the following stages a) demethylation of 6-methoxy-2-(4-methoxyphenyl)benzo[b]thiophene in pyridine and hydrochloric acid to obtain 6-hydroxy­2-(4-hydroxyphenyl)benzo[b]thiophene in pyridine hydrochloride, b) acetylation of 6-hydroxy-2-(4­hydroxyphonyl)benzo[b]thiophene with an acetylating agent to obtain the corresponding 6-acetoxy-2-(4 acetoxyphenyl)benzo[b]thiophene, c) acylation of 6-acetoxy-2-(4-acetoxyphonyl)benzo[b]thlophene with 4-(2 piperidinoethoxy)benzoylchloride hydrochloride with aluminium trichloride in halogenated solvent to obtain 6-acetoxy-2-(4­acetoxyphenyl)-3-[4-(2 piperidinoethoxy)benzoyl]-benzo[b]thiophene, d) hydrolysis of 6-acetoxy-2-(4-acetoxyphenyl)-3-[4-(2-piperidinoethoxy)benzoyll benzo[b]thiophene according to the following operating conditions: dl) treatment of 6-acetoxy-2-(4-acetoxyphonyl)-3-[4-(2­piperidinoethoxy)benzoyl]benzo[b]thiophene with alkaline hydroxide in alcohol solvent, d2) acidification of the product obtained in the preceding stage (dl) with a strong acid, to obtain the corresponding raloxifene salt with the strong acid, characterised in that the strong acid used in stage (d2) is concentrated hydrochloric acid.

    Abstract translation: 制备纯度大于98％的雷洛昔芬盐酸盐和低铝含量的方法，包括以下步骤：a）将6-甲氧基-2-（4-甲氧基苯基）苯并[b]噻吩在吡啶和盐酸中脱甲基，得到6-羟基-2- - （4-羟基苯基）苯并[b]噻吩在吡啶盐酸盐中，b）用乙酰化剂将6-羟基-2-（4-羟基丙基）苯并[b]噻吩乙酰化得到相应的6-乙酰氧基-2-（4 乙酰氧基苯基）苯并[b]噻吩，c）用4-（2-哌啶子基乙氧基）苯甲酰氯盐酸盐与氯化铝在卤化溶剂中酰化6-乙酰氧基-2-（4-乙酰氧基丙基）苯并[b]乙烯基，得到6-乙酰氧基-2 - （4-乙酰氧基苯基）-3- [4-（2-哌啶子基乙氧基）苯甲酰基] - 苯并[b]噻吩，d）6-乙酰氧基-2-（4-乙酰氧基苯基）-3- [4-（2-哌啶子基乙氧基） 苯甲酰基苯并[b]噻吩根据以下操作条件：dl）处理6-乙酰氧基-2-（4-乙酰氧基丙基）-3- [4-（2-哌啶基乙氧基）苯甲酰基]苯并[b]噻吩 用碱性氢氧化物在醇溶剂中，d2）用强酸酸化前一阶段（dl）中得到的产物，得到与强酸相应的雷洛昔芬盐，其特征在于阶段（d2）中使用的强酸为 浓盐酸。

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