公开(公告)号：US20140350281A1

公开(公告)日：2014-11-27

申请号：US14454982

申请日：2014-08-08

Applicant: Vertex Pharmaceuticals Incorporated

Inventor： John DeMattei ,  Adam R. Looker ,  Bobbianna J. Neubert-Langille ,  Martin Trudeau ,  Stefanie Roeper ,  Michael P. Ryan ,  Dahrika Milfred Yap Guerette ,  Brian R. Krueger ,  Peter Diederik Jan Grootenhuis ,  Fredrick F. Van Goor ,  Martyn Curtis Botfield ,  Gregor Zlokarnik

IPC: C07C213/02 ,  C07C68/02 ,  C07C201/08

CPC classification number: C07C205/43 ,  C07C68/02 ,  C07C69/96 ,  C07C201/08 ,  C07C213/02 ,  C07C229/66 ,  C07D215/233 ,  C07D215/56 ,  G01N33/5041 ,  G01N33/6872 ,  Y02P20/55

Abstract: The invention provides a process for the preparation of a compound of Formula 1, comprising coupling a carboxylic acid of Formula 2 with an aniline of Formula 3 in the presence of a coupling agent.

公开(公告)号：US20130253233A1

公开(公告)日：2013-09-26

申请号：US13427688

申请日：2012-03-22

Applicant: Michael Gattrell

Inventor： Michael Gattrell

IPC: C07C201/08

CPC classification number: C07C201/08 ,  C07C205/06

Abstract: A process for continuous adiabatic nitration of toluene to mononitrotoluene (MNT). The process yields a product quality of MNT that is comparable to that obtained by isothermal production. The process uses excess toluene, with the reaction rate being controlled to maintain a residual of 0.003-0.102 wt % nitric acid in the spent acid and an orange to red color of the spent acid. Further process conditions include re-concentrated sulfuric acid at 83 to 99 degrees C. with a concentration of sulfuric acid from 66 to 70.5 wt %. This is mixed with nitric acid to generate a mixed acid with 1.0 to 3.8 wt % nitric acid and toluene is added at a rate of 1.1 to 1.71 moles toluene/mole nitric acid. The reactants are mixed in a reactor with an overall average mixing intensity of 5.8 to 19 W/kg of contained solution.

Abstract translation: 将甲苯连续绝热硝化成单硝基甲苯（MNT）的方法。 该方法产生与通过等温生产获得的MNT相当的MNT的产品质量。 该方法使用过量的甲苯，控制反应速率以维持废酸中的0.003-0.102重量％的硝酸残留量和废酸的橙色至红色。 进一步的工艺条件包括在83至99℃下的浓硫酸，浓度为66至70.5重量％的硫酸。 将其与硝酸混合以产生具有1.0至3.8重量％硝酸的混合酸，并以1.1至1.71摩尔甲苯/摩尔硝酸的速率加入甲苯。 反应物在反应器中混合，总体平均混合强度为5.8至19W / kg的所含溶液。

公开(公告)号：US08415514B2

公开(公告)日：2013-04-09

申请号：US12879799

申请日：2010-09-10

Applicant: Daniel M. Trauth

Inventor： Daniel M. Trauth

IPC: C07C201/06 ,  C07C201/08

CPC classification number: B01J19/0053 ,  B01J10/00 ,  B01J19/02 ,  B01J19/30 ,  B01J19/32 ,  B01J2219/00164 ,  B01J2219/029 ,  B01J2219/30215 ,  C07C201/08 ,  C07C205/02

Abstract: Disclosed are a process and an apparatus for synthesizing nitroalkanes by reaction of a hydrocarbon feedstock with aqueous nitric acid. By using an isothermal reactor with multiple input ports for aqueous nitric acid, a hydrocarbon feedstock may be sequentially exposed to a plurality of flows of aqueous nitric acid as it flows through the reactor.

Abstract translation: 公开了通过烃原料与硝酸水溶液反应来合成硝基烷烃的方法和装置。 通过使用具有用于硝酸水溶液的多个输入端口的等温反应器，烃原料可以在流过反应器时依次暴露于多个硝酸水溶液。

公开(公告)号：US20130018210A1

公开(公告)日：2013-01-17

申请号：US13636478

申请日：2011-02-17

Applicant: Alfred A. Guenkel ,  Sergio Berretta

Inventor： Alfred A. Guenkel ,  Sergio Berretta

IPC: C07C201/08 ,  B01J19/00

CPC classification number: C07C201/16 ,  Y02P20/582 ,  C07C205/06 ,  C07C205/12

Abstract: A method and apparatus for removing non-aromatic impurities from non-nitrated aromatic reactant in a nitration production process, in which process an aromatic reactant is nitrated (100) to produce a nitrated aromatic product using a molar excess of the aromatic reactant, and non-nitrated aromatic reactant is recovered (102) from the produced nitrated aromatic product and is recycled (104) for use in the nitration production process. A portion of the removed excess non-nitrated aromatic reactant is diverted (106) and subjected to nitration (108). The nitrated stream may be further processed by separating out the spent acids (110) and the non-aromatic impurities (116). These streams may be sent (114, 118) to a suitable location in the nitration production train.

Abstract translation: 一种用于在硝化生产过程中从非硝化芳族反应物除去非芳族杂质的方法和装置，其中芳族反应物被硝化（100）以产生使用摩尔过量的芳族反应物的硝化芳族产物， 硝酸芳香族反应物（102）从所生产的硝化芳香族产物中回收（102）并循环使用（104），用于硝化生产过程。 去除的过量非硝化芳族反应物的一部分被转移（106）并进行硝化（108）。 可以通过分离废酸（110）和非芳族杂质（116）来进一步处理硝化物流。 这些流可以被发送（114,118）到硝化生产列车中的合适位置。

公开(公告)号：US20100160695A1

公开(公告)日：2010-06-24

申请号：US12634772

申请日：2009-12-10

Applicant: JOACHIM C. RITTER

Inventor： JOACHIM C. RITTER

IPC: C07C201/08

CPC classification number: C07C201/08 ,  C07C205/12

Abstract: An improved process is provided for the preparation of 2,6-dihalo-3,5-dinitrotoluene by the nitration of 2,6-dihalotoluene. The direct isolation of highly pure 2,6-dihalo-3,5-dinitrotoluene is accomplished without a water or ice quench, by providing at least one equivalent of SO3 during the reaction, slow crystallization, and isolation of product from a cold crystal slurry.

Abstract translation: 提供了通过2,6-二卤代甲苯硝化制备2,6-二卤代-3,5-二硝基甲苯的改进方法。 通过在反应期间提供至少一当量的SO 3，缓慢结晶并从冷结晶浆中分离产物，直接分离高纯度的2,6-二卤代-3,5-二硝基甲苯，无需水或冰骤冷 。

公开(公告)号：US06930214B2

公开(公告)日：2005-08-16

申请号：US10883820

申请日：2004-07-06

Applicant: Tamaki Shimizu

Inventor： Tamaki Shimizu

IPC: C07C201/08 ,  C07C205/11 ,  C07J73/00 ,  C07J75/00 ,  C07C205/00 ,  C07D221/18

CPC classification number: C07J75/00 ,  C07C201/08 ,  C07J73/00 ,  C07C205/11

Abstract: A process to produce 2,5-bis(trifluoromethyl)nitrobenzene in a high yield from an industrially easily available material by using a substance with which the reaction operation is simple and handling is easy, with a small number of steps under moderate reaction conditions, is provided. 1,4-bis(trifluoromethyl)benzene is nitrated by means of nitric acid in a solvent comprising as an essential component an acid selected from sulfuric acid having a sulfuric acid concentration of from 91 to 100 mass % and fuming sulfuric acid having a sulfur trioxide concentration of higher than 0 mass % and at most 20 mass %.

Abstract translation: 通过使用反应操作简单并且处理容易的物质，在中等反应条件下以少量的步骤从工业上容易获得的材料中以高产率制备2,5-双（三氟甲基）硝基苯的方法， 被提供。 1,4-二（三氟甲基）苯通过硝酸在含有选自硫酸浓度为91〜100质量％的硫酸和三氧化硫的发烟硫酸作为必需成分的溶剂中进行硝化 浓度高于0质量％，最多为20质量％。

公开(公告)号：US20050113596A1

公开(公告)日：2005-05-26

申请号：US10972575

申请日：2004-10-25

Applicant: Thierry Schlama ,  Armand Mettling ,  Philippe Karrer

Inventor： Thierry Schlama ,  Armand Mettling ,  Philippe Karrer

IPC: C07B61/00 ,  C07C67/31 ,  C07C69/712 ,  C07C69/734 ,  C07C201/08 ,  C07C205/37 ,  C07C205/44 ,  C07C319/14 ,  C07C319/20 ,  C07C323/52 ,  C07D307/79 ,  C07D333/54 ,  C07C323/22 ,  C07C25/53

CPC classification number: C07D307/79 ,  C07C67/31 ,  C07C201/12 ,  C07C205/37 ,  C07D333/54 ,  C07C69/712

Abstract: The invention concerns novel nitroaromatic compounds of general formula (I′) wherein: R, R′1, R2, Z and n are as defined in claim 38. The invention also concerns a method for preparing nitroaromatic compounds nitrated in position 4. The invention further concerns the use of said compounds for preparing heterocyclic benzofuran or benzothiophene derivatives nitrated in position 5. The invention concerns particularly the preparation of 2-alkyl-5-nitrobezofuran

Abstract translation: 本发明涉及通式（I'）的新型硝基芳族化合物，其中：R，R'1，R2，Z和n如权利要求38中所定义。本发明还涉及制备位置4中硝化芳族化合物的方法。本发明 进一步关于所述化合物用于制备位置5中硝化的杂环苯并呋喃或苯并噻吩衍生物的用途。本发明特别涉及2-烷基-5-硝基吩呋呋喃的制备

公开(公告)号：US6160127A

公开(公告)日：2000-12-12

申请号：US115427

申请日：1998-07-15

Applicant: Giuseppe Prota ,  Gottfried Wenke

Inventor： Giuseppe Prota ,  Gottfried Wenke

IPC: C07C201/08 ,  C07C205/22 ,  C07C205/43 ,  C07D209/08 ,  C07D209/04 ,  C07D209/12

CPC classification number: C07D209/08 ,  C07C201/08 ,  C07C201/12 ,  C07C205/22 ,  C07C205/04 ,  C07C205/06

Abstract: A process for the preparation of 5,6-disubstituted indoles in which a 4-5-disubstituted-2,.beta.-nitrostyrene is subjected to a reductive cyclization in the presence of a water soluble dithionite salt.

Abstract translation: 制备5,6-二取代吲哚的方法，其中4-5-二取代-2β-硝基苯乙烯在水溶性连二亚硫酸盐存在下进行还原环化。

公开(公告)号：US6034287A

公开(公告)日：2000-03-07

申请号：US188589

申请日：1998-11-09

Applicant: Boyapati Manoranjan Choudary ,  Mutyala Sateesh ,  Mannepalli Lakshmi Kantam ,  Kottapalli Koteswara Rao ,  Kompella Vishweshwar Ram Prasad ,  Kondapuram Vijaya Raghavan

Inventor： Boyapati Manoranjan Choudary ,  Mutyala Sateesh ,  Mannepalli Lakshmi Kantam ,  Kottapalli Koteswara Rao ,  Kompella Vishweshwar Ram Prasad ,  Kondapuram Vijaya Raghavan

IPC: B01J21/16 ,  B01J29/08 ,  B01J29/18 ,  B01J29/40 ,  B01J29/70 ,  C07C201/08 ,  C07C205/06 ,  C07C205/12 ,  C07C205/37 ,  C07C205/00

CPC classification number: C07C201/08 ,  B01J29/7007

Abstract: The present invention relates to a process for the production of nitroarenes with high para-selectivity from monosubstituted aromatic hydrocarbons using aluminosilicates as catalysts, which comprises nitration of monosubstituted aromatic hydrocarbons using aluminosilicates of different ratios wherein Si/Al ranges between 5 to 1000 and the said aluminosilicates being manifested in the form of variety of zeolites and K10 montmorillonite as catalysts using nitric acid in the molar ratio of nitric acid to monosubstituted aromatic hydrocarbons ranging between 0.25 to 2.5 at a temperature in the range of 30-160.degree. C. for a period ranging between 0.25 to 3.0 h and followed by continuous removal of water formed from the reaction mixture with a Dean-Stark apparatus and recovery of the product mixture by concentration of the reaction mixture after separation of the catalyst by filtration.

Abstract translation: 本发明涉及一种使用铝硅酸盐作为催化剂从单取代芳族烃生产具有高对选择性的硝基芳烃的方法，该方法包括使用不同比率的硅铝酸盐硝化单取代芳烃，其中Si / Al在5至1000之间，所述 铝硅酸盐以各种沸石和K10蒙脱石的形式表现为催化剂，使用硝酸在硝酸与单取代芳烃的摩尔比在0.25至2.5之间的温度范围为30-160℃，持续一段时间 在0.25至3.0小时之间，然后用Dean-Stark装置连续除去由反应混合物形成的水，并通过过滤分离催化剂后浓缩反应混合物回收产物混合物。

公开(公告)号：US5907062A

公开(公告)日：1999-05-25

申请号：US974104

申请日：1997-11-19

Applicant: Alberto Villanti ,  Giacomo Ravetta

Inventor： Alberto Villanti ,  Giacomo Ravetta

IPC: B01J27/24 ,  B01J31/02 ,  C07B61/00 ,  C07C201/08 ,  C07C205/23 ,  C07C209/76 ,  C07C211/52

CPC classification number: C07C209/76

Abstract: A continuous process for the dinitration of alkyl-substituted derivatives of phenol and aniline, using nitric acid substantially free of sulphuric acid, characterized in which the dinitration is conducted in a single step in a tubular reactor in the presence of a catalytically-effective amount of a catalyst capable of reacting with the nitric acid to form nitrous acid in situ.

Abstract translation: 使用基本上不含硫酸的硝酸对苯酚和苯胺的烷基取代的衍生物进行二硝化的连续方法，其特征在于在催化有效量的条件下，在管式反应器中，在一个步骤中进行二硝化反应 能够与硝酸反应以在原位形成亚硝酸的催化剂。