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    FLUORINATION METHOD
    4.
    发明申请
    FLUORINATION METHOD 审中-公开
    荧光法

    公开(公告)号：WO2015140572A1

    公开(公告)日：2015-09-24

    申请号：PCT/GB2015/050831

    申请日：2015-03-20

    Applicant: ISIS INNOVATION LIMITED

    Inventor： GOUVERNEUR, Veronique ,  TREDWELL, Matthew ,  PRESHLOCK, Sean

    IPC: C07B59/00 ,  C07F5/04

    CPC classification number: C07B59/002 ,  C07B59/00 ,  C07B59/001 ,  C07B2200/05 ,  C07C17/361 ,  C07C37/62 ,  C07C41/22 ,  C07C45/65 ,  C07C67/317 ,  C07C201/12 ,  C07C209/74 ,  C07C231/12 ,  C07C253/30 ,  C07C303/40 ,  C07D209/08 ,  C07D215/18 ,  C07D277/30 ,  C07D295/073 ,  C07D295/16 ,  C07F5/025 ,  C07F5/04 ,  Y02P20/55

    Abstract: The present invention relates to a process for producing an organic compound comprising an 18 F atom. The compounds comprising an 18 F can be useful as PET ligands for use in diagnostics and/or scanning. The process of the invention comprises treating an organoboron compound, which organoboron compound comprises a boron atom bonded to an sp 2 hybridised carbon atom, with (i) 18 F – and (ii) a copper compound. The invention also provides the use of an organoboron compound, which organoboron compound comprises a boron atom bonded to an sp 2 hybridised carbon atom, in a process for producing an organic compound comprising an 18 F atom, which process comprises treating the organoboron compound with (i) 18 F – and (ii) a copper compound. The invention also provides a compound of formula (XXXVII): wherein: each PG A is independently H or an alcohol protecting group; PG B is H or a carboxylic acid protecting group; each PG C is independently an amine protecting group; Z is a group selected from a boronic ester group, a boronic acid group, a borate group, and a trifluoroborate group; and a is an integer from 0 to 4.

    Abstract translation: 本发明涉及一种制备包含18F原子的有机化合物的方法。 包含18F的化合物可用作用于诊断和/或扫描的PET配体。 本发明的方法包括处理有机硼化合物，该有机硼化合物包含与sp2杂化的碳原子键合的硼原子与（i）18 F-和（ii）铜化合物。 本发明还提供有机硼化合物的用途，该有机硼化合物包含与sp2杂化的碳原子键合的硼原子，所述有机硼化合物在制备包含18 F原子的有机化合物的方法中，所述方法包括用（i） 18F-和（ii）铜化合物。 本发明还提供式（XXXVII）化合物：其中：各PGA独立地为H或醇保护基; PGB是H或羧酸保护基; 每个PGC独立地是胺保护基; Z是选自硼酸酯基，硼酸基，硼酸酯基和三氟硼酸酯基的基团; a为0〜4的整数。

    PROCESS FOR PREPARATION OF HERBICIDAL CARBOXYLIC ACID SALTS
    5.
    发明申请
    PROCESS FOR PREPARATION OF HERBICIDAL CARBOXYLIC ACID SALTS 审中-公开
    制备除草剂羧酸盐的方法

    公开(公告)号：WO2015062286A1

    公开(公告)日：2015-05-07

    申请号：PCT/CN2014/080265

    申请日：2014-06-19

    Applicant: ROTAM AGROCHEM INTERNATIONAL COMPANY LIMITED

    Inventor： BRISTOW, James, Timothy

    IPC: C07C51/41 ,  C07C59/70 ,  C07C63/08 ,  A01N37/10 ,  A01N39/02 ,  A01N43/70

    CPC classification number: C07C51/412 ,  A01N25/12 ,  A01N33/08 ,  A01N37/10 ,  A01N37/40 ,  A01N39/04 ,  A01N43/40 ,  A01N43/42 ,  C07C51/42 ,  C07C51/47 ,  C07C59/68 ,  C07C65/21 ,  C07C213/08 ,  C07C215/08 ,  C07D213/79 ,  C07D213/803 ,  C07D215/18

    Abstract: A process for preparing a herbicidally active carboxylic acid salt is disclosed, the process comprising the steps of: i) combining a carboxylic acid with a high-boiling, water-immiscible organic solvent to obtain a solution or slurry; ii) treating the solution or slurry produced in step (i) with a base to form a carboxylic acid salt; iii) removing solvent from the mixture produced in step (ii) to obtain a carboxylic acid salt cake; and v) drying the cake obtained in step (iii). The process is particularly suitable for preparing a salt of dicamba. A process for preparing dicamba-sodium comprises: (1) dissolving a carboxylic acid consisting essentially of dicamba in a high-boiling water-immiscible inert organic solvent to get a solution or slurry; (2) treating the dicamba solution or slurry in Step 1 with a base selected from sodium hydroxide, sodium bicarbonate and mixtures thereof, at a molar ratio of 1:0.97±0.6% to form dicamba-sodium; (3) centrifuging the reaction mixture in Step 2 to obtain dicamba-sodium salt cake; and (4) drying the dicamba-sodium cake obtained in Step 3 to get a dry dicamba- sodium consistently having a pH value between about 7 and 10 when dissolved in water.

    Abstract translation: 公开了一种制备除草活性羧酸盐的方法，该方法包括以下步骤：i）将羧酸与高沸点的与水不混溶的有机溶剂混合以获得溶液或浆料; ii）用碱处理在步骤（i）中产生的溶液或浆料以形成羧酸盐; iii）从步骤（ii）中制备的混合物中除去溶剂，得到羧酸盐饼; 和v）干燥步骤（iii）中获得的饼。 该方法特别适用于制备麦草畏的盐。 制备麦草畏钠的方法包括：（1）将基本上由麦草畏草组成的羧酸溶解在高沸水不溶混的惰性有机溶剂中以得到溶液或浆液; （2）以1：0.97±0.6％的摩尔比，用选自氢氧化钠，碳酸氢钠和其混合物的碱处理步骤1中的麦草畏溶液或淤浆，形成麦草畏; （3）在步骤2中离心反应混合物，得到麦草畏钠盐饼; 和（4）干燥步骤3中获得的麦草畏钠饼以获得当溶解在水中时，一般具有约7至10的pH值的干燥的麦角氨酸钠。

    AN IN-SITU PROCESS FOR THE PREPARATION OF HIGHLY PURE MONTELUKAST SODIUM
    6.
    发明申请
    AN IN-SITU PROCESS FOR THE PREPARATION OF HIGHLY PURE MONTELUKAST SODIUM 审中-公开
    用于制备高纯度蒙特梭菌钠的现场方法

    公开(公告)号：WO2014118796A1

    公开(公告)日：2014-08-07

    申请号：PCT/IN2013/000312

    申请日：2013-05-13

    Applicant: MELODY HEALTHCARE PVT. LTD.

    Inventor： PATEL, Dayabhai Somabhai ,  GHOGARE, Anil Balkrishna ,  VISHE, Kishor Tukaram

    IPC: C07D215/18 ,  A61K31/47 ,  A61P11/06

    CPC classification number: C07D215/18

    Abstract: The present invention disclosed herein is a cost effective, in-situ process for the preparation of montelukast or its pharmaceutically acceptable salts of formula (1) by reacting optically pure (S)-1-{3-[2-(7-chloroquinolin-2-yl)ethylene]-phenyl}-3-[2-(1-hydroxy-1-methyl ethyl) phenyl]-propan-I-ol with methane sulfonyl chloride to afford mesylate derivative of formula (2) substantially free of impurities; followed by insitu condensing the same with disodium salt of mercapto-cyclopropyl acetic acid of formula (3) to afford montelukast free acid in good yield and purity, then converting the montelukast free acid into its substituted amine salt of formula (4). Further the montelukast substituted amine is converted into its pharmaceutically acceptable salt.

    Abstract translation: 本文公开的本发明是通过使光学纯的（S）-1- {3- [2-（7-氯喹啉-2-基） 吡啶-2-基）乙烯] - 苯基} -3- [2-（1-羟基-1-甲基乙基）苯基] - 丙-1-醇与甲磺酰氯反应，得到基本上不含杂质的式（2）的甲磺酸酯衍生物 ; 然后将其与式（3）的巯基 - 环丙基乙酸的二钠盐相同地进行缩合，得到良好的产率和纯度的孟鲁司特游离酸，然后将孟鲁司特游离酸转化为式（4）的取代的胺盐。 此外，孟鲁司特胺取代的胺被转化成其药学上可接受的盐。

    QUINOLINE DERIVATIVES AND METHOD FOR PRODUCING AND USING SAME
    8.
    发明申请
    QUINOLINE DERIVATIVES AND METHOD FOR PRODUCING AND USING SAME 审中-公开
    喹啉衍生物及其制备方法和使用方法

    公开(公告)号：WO2013039428A3

    公开(公告)日：2013-05-10

    申请号：PCT/RU2012000725

    申请日：2012-09-04

    Applicant: ZAKRYTOE AKTSIONERNOE OBSCHESTVO PHARM SINTEZ ,  NAZARENKO ANNA BORISOVNA ,  FEDOROV VLADIMIR EGOROVICH ,  ILIIN VADIM EGOREVICH ,  OMELKOV ANTON VLADIMIROVICH ,  RUCHKO EVSEJ ALEKSANDROVICH

    Inventor： NAZARENKO ANNA BORISOVNA ,  FEDOROV VLADIMIR EGOROVICH ,  ILIIN VADIM EGOREVICH ,  OMELKOV ANTON VLADIMIROVICH ,  RUCHKO EVSEJ ALEKSANDROVICH

    IPC: C07D215/18 ,  A61K31/47 ,  A61P31/06

    CPC classification number: C07D215/18 ,  C07D215/20 ,  C07D491/056

    Abstract: The present invention relates to novel quinoline derivatives, such as substituted 1-(2-chloroquinolin-3-yl)-4-dimethylamino-2-(naphthalen-1-yl)-1- phenylbutan-2-ols, to a method for producing same, and also to the use thereof as antimycobacterial agents, in particular to 5,6,7-substituted 1-(2-chloroquinolin-3-yl)-4-dimethylamino-2-(naphthalen-1-yl)-1- phenylbutan-2-ols of general formula (I), where R1 is Н or methoxy, R2 is Н, methoxy or -O-(CH2)n-O-, R3 is Н, methoxy or -O-(CH2)n-O-, n=1-2, and also to the pharmaceutically acceptable salts thereof with acids which exhibit activity in relation to mycobacteria. The invention also relates to a method for producing compounds of formula (I), which consists in interacting corresponding arylquinolines with an aromatic ketone and using said compounds as an active principle in the creation of anti-tubercular medicinal preparations.

    Abstract translation: 本发明涉及新颖的喹啉衍生物，例如取代的1-（2-氯喹啉-3-基）-4-二甲基氨基-2-（萘-1-基）-1-苯基丁-2-醇， 以及作为抗分枝杆菌剂的用途，特别是5,6,7-取代的1-（2-氯喹啉-3-基）-4-二甲基氨基-2-（萘-1-基）-1 （I）的苯基丁-2-醇，其中R 1是Н或甲氧基，R 2是Н，甲氧基或-O-（CH 2）n O-，R 3是Н，甲氧基或-O-（CH 2）n O-， n = 1-2，并且其药学上可接受的盐与表现出与分枝杆菌有关的活性的酸。 本发明还涉及一种制备式（I）化合物的方法，其包括将相应的芳基喹啉与芳族酮相互作用，并使用所述化合物作为抗结核药物制剂的产生的活性成分。

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