公开(公告)号：US5700934A

公开(公告)日：1997-12-23

申请号：US616742

申请日：1996-03-15

Applicant: Henricus F. W. Wolters ,  Samuel L. Lane ,  Wim Buijs ,  Nicolaas F. Haasen ,  Frank E. Herkes

Inventor： Henricus F. W. Wolters ,  Samuel L. Lane ,  Wim Buijs ,  Nicolaas F. Haasen ,  Frank E. Herkes

IPC: C07D201/08

CPC classification number: C07D201/08

Abstract: A process for the preparation of .epsilon.-caprolactam and .epsilon.-caprolactam precursors, starting from the corresponding 5-formylvalerate ester, ammonia and hydrogen in the presence of a hydrogenation catalyst is disclosed, wherein in a step (a) 5-formylvalerate ester is reacted with ammonia under non-hydrogenating conditions, and in a step (b) the reaction product obtained in step (a) is converted to .epsilon.-caprolactam and the .epsilon.-caprolactam precursor(s) under hydrogenating conditions, in the presence of ammonia.

Abstract translation: 公开了在氢化催化剂存在下从相应的5-甲酰基戊酸酯，氨和氢开始制备ε-己内酰胺和ε-己内酰胺前体的方法，其中在步骤（a）中，使5-甲酰基戊酸酯反应 在非氢化条件下用氨，并且在步骤（b）中，在氨的存在下，在氢化条件下将步骤（a）中获得的反应产物转化成ε-己内酰胺和ε-己内酰胺前体。

公开(公告)号：US5393888A

公开(公告)日：1995-02-28

申请号：US204577

申请日：1994-03-02

Applicant: Francis B. Minnock ,  Paul D. Taylor

Inventor： Francis B. Minnock ,  Paul D. Taylor

IPC: C07D207/26 ,  C07D207/267 ,  C07D201/08

CPC classification number: C07D207/267

Abstract: This invention relates to a liquid phase process for producing 2-pyrrolidone in high yield and selectivity in the absence of catalyst and extraneous solvents which involves contacting ammonia with butyrolactone in a molar ratio of from 0.5:1 to 0.85:1 at high temperature and pressure sufficient to maintain the liquid phase.

Abstract translation: 本发明涉及在不存在催化剂和外来溶剂的情况下以高产率和选择性生产2-吡咯烷酮的液相方法，该方法包括使氨与丁酸内酯在摩尔比为0.5:1至0.85:1的高温和高压下接触 足以维持液相。

公开(公告)号：US5276165A

公开(公告)日：1994-01-04

申请号：US982300

申请日：1992-11-25

Applicant: Hans-Juergen Weyer ,  Rolf Fischer

Inventor： Hans-Juergen Weyer ,  Rolf Fischer

IPC: B01J21/04 ,  B01J23/28 ,  B01J23/34 ,  B01J23/72 ,  B01J23/75 ,  C07B61/00 ,  C07D201/02 ,  C07D201/08 ,  C07D207/26 ,  C07D207/267 ,  C07D209/46 ,  C07D209/64 ,  C07D223/10 ,  C07D225/02 ,  C07D207/12 ,  C07D221/06

CPC classification number: C07D201/02 ,  C07D201/08 ,  C07D207/267

Abstract: A process for the preparation of N-substituted lactams of the formula I ##STR1## where Z is C.sub.2 - to C.sub.10 -alkylene, C.sub.7 - to C.sub.12 -aralkylene, phenylene or naphthylene, andR.sup.1 is C.sub.1 - to C.sub.20 -alkyl, C.sub.6 - to C.sub.10 -aryl or C.sub.7 - to C.sub.12 -aralkyl,by hydrogenating a compound of the formula II ##STR2## where W is C.sub.2 - to C.sub.10 -alkylene, C.sub.2 - to C.sub.10 -alkenylene, C.sub.7 - to C.sub.12 -aralkylene, phenylene or naphthylene, andX and Y together form an oxa or imido bridge of the formula ##STR3## or alternatively are identical or different and are hydroxyl, C.sub.1 - to C.sub.20 -alkoxy, C.sub.6 - to C.sub.10 -aryloxy or C.sub.7 - to C.sub.12 -aralkoxy, and, if X and Y are different, Y, in addition to the abovementioned meanings, may also be hydrogen,at superatmospheric pressure and at elevated temperature in the presence of a catalyst and in the presence of an amine, which comprises using a secondary and/or tertiary amine of the formula IIINH.sub.n R.sub.3-n .sup.1where R.sup.1 is as defined above and n is 0 or 1, or a mixture of a secondary and/or teritary amine of this type with a primary amine of the formula IVR.sup.1 --NH.sub.2 (IV)as the starting material, and carrying out the reaction with addition of water and/or ammonia.

Abstract translation: 制备式I的N-取代的内酰胺的方法（I）其中Z为C 2至C 10亚烷基，C 7至C 12 - 亚芳基，亚苯基或亚萘基，R 1为C 1 -C 20烷基 C 6 -C 10 - 芳基或C 7 - 至C 12 - 芳烷基，其中W是C 2 - 至C 10 - 亚烷基，C 2至C 10亚烯基，C 7 - 至C 12 - 亚烷基， - 亚烷基，亚苯基或亚萘基，X和Y一起形成下式的氧杂或亚氨基桥，或者可选地相同或不同，为羟基，C 1至C 20 - 烷氧基，C 6至C 10 - 芳氧基或C 7 - 对于C 12 - 芳烷氧基，并且如果X和Y不同，除了上述含义之外，Y还可以是氢，在超大气压和升高的温度下，在催化剂的存在下和在胺的存在下， 包括使用式III NH n R 3-n 1的仲和/或叔胺，其中R 1如上定义并且n为0或1，或者该仲胺和/或叔胺的混合物 以式ⅣR-NH2（Ⅳ）的伯胺为起始原料，并加入水和/或氨进行反应。

公开(公告)号：US4767857A

公开(公告)日：1988-08-30

申请号：US133735

申请日：1987-12-16

Applicant: Franz Merger ,  Claus-Ulrich Priester ,  Rolf Fischer ,  Manfred Sauerwald

Inventor： Franz Merger ,  Claus-Ulrich Priester ,  Rolf Fischer ,  Manfred Sauerwald

IPC: C07D201/08

CPC classification number: C07D201/08

Abstract: Caprolactam is prepared by heating a 6-aminocaproic ester at 100.degree.-320.degree. C. in the presence of a reaction medium comprising an aromatic hydrocarbon which is liquid under reaction conditions and has a boiling point from 80.degree. to 240.degree. C., and isolating caprolactam from the reaction medium.

Abstract translation: 在含有在反应条件下为液体并且沸点为80-240℃的芳族烃的反应介质存在下，在100-320℃下加热6-氨基己酸酯制备己内酰胺， 从反应介质中分离己内酰胺。

公开(公告)号：US4730040A

公开(公告)日：1988-03-08

申请号：US7788

申请日：1987-01-28

Applicant: Uwe Vagt ,  Rolf Fischer ,  Franz Merger ,  Hans-Martin Hutmacher

Inventor： Uwe Vagt ,  Rolf Fischer ,  Franz Merger ,  Hans-Martin Hutmacher

IPC: C07D223/04 ,  C07D201/08

CPC classification number: C07D201/08

Abstract: .epsilon.-caprolactam is prepared by a process in which(a) a 5-formylvalerate is reacted with water in the presence of an acidic agent at from 30.degree. to 200.degree. C.,(b) the 5-formylvaleric acid thus obtained is reacted with excess ammonia and hydrogen in the presence of a hydrogenation catalyst and of a solvent which is inert under the reaction conditions, at from 50.degree. to 150.degree. C. under superatmospheric pressure, and(c) after the ammonia has been separated off, the resulting solution of 6-aminocaproic acid is heated to 150.degree.-370.degree. C. and the caprolactam formed is isolated.

Abstract translation: ε-己内酰胺通过以下方法制备：（a）在30℃至200℃下，在酸性试剂存在下，使5-甲酰基戊酸酯与水反应，（b）将所得的5-甲酰基戊酸反应 在氢化催化剂和在反应条件下为惰性的溶剂中，在超大气压下，在50-150℃下，过量的氨和氢，和（c）氨分离后， 将得到的6-氨基己酸溶液加热至150-370℃，形成己内酰胺。

公开(公告)号：US4647661A

公开(公告)日：1987-03-03

申请号：US845122

申请日：1986-03-27

Applicant: Paolo Senni ,  Leandro Zuliani ,  Sergio Ferruzzi

Inventor： Paolo Senni ,  Leandro Zuliani ,  Sergio Ferruzzi

IPC: C07D201/16 ,  C07D201/08 ,  C07D201/10

CPC classification number: C07D201/08

Abstract: A method of preparing .omega.-lactams, in particular caprolactam, comprising: a step of premixing cycloaliphatic acids having the formula ##STR1## where n=3-13, with a dehydrating agent; the first step of reaction with a nitrosating agent; the second step of reaction with the addition of a very small amount of water corresponding to a molar ratio U=H.sub.2 O/SO.sub.3 within the 0.1 to 0.9 range; and the step of reclaiming the unreacted cycloaliphatic acid. The method affords improved output from the lactamization reaction and reduced byproducts.

Abstract translation: 一种制备ω-内酰胺，特别是己内酰胺的方法，包括：将具有式“IMAGE”的其中n = 3-13的脂环族酸与脱水剂预混合的步骤; 与亚硝化剂反应的第一步; 反应的第二步骤是加入相当于0.1至0.9范围内的摩尔比U = H 2 O / SO 3的非常少量的水; 以及回收未反应的脂环族酸的步骤。 该方法提供了来自内酰胺化反应的改进的产物和减少的副产物。

公开(公告)号：US4625023A

公开(公告)日：1986-11-25

申请号：US771853

申请日：1985-09-03

Applicant: Frank Mares ,  Reginald Y. Tang ,  James E. Galle ,  Rose M. Federici

Inventor： Frank Mares ,  Reginald Y. Tang ,  James E. Galle ,  Rose M. Federici

IPC: C07D201/08 ,  C07D223/10

CPC classification number: C07D201/08

Abstract: Process for the selective conversion of dinitriles into the corresponding lactam by treating the dinitrile with an effective amount of a hydrogenation catalyst such as copper chromite in combination with a co-catalyst, such as titania, at a temperature in the range of from about 200.degree. C. to about 400.degree. C. and at a pressure of at least 50 kPa in the presence of water and hydrogen.

Abstract translation: 通过用有效量的氢化催化剂如亚铬酸铜与助催化剂如二氧化钛的组合处理二腈，将二腈选择性转化成相应的内酰胺的方法，温度范围为约200℃ 在约400℃下和在水和氢气存在下在至少50kPa的压力下进行。

公开(公告)号：US4599199A

公开(公告)日：1986-07-08

申请号：US696796

申请日：1985-01-31

Applicant: Hugo Fuchs

Inventor： Hugo Fuchs

IPC: C07D201/08

CPC classification number: C07D201/08

Abstract: Caprolactam is obtained by treating .epsilon.-aminocaproic acid with steam at elevated temperatures in the presence of a catalyst by a process in whcih .epsilon.-aminocaproic acid is introduced into a fluidized alumina bed and treated in the presence of steam at from 290.degree. to 400.degree. C.

Abstract translation: 己内酰胺通过在催化剂存在下在高温下用蒸汽处理ε-氨基己酸获得，其中将ε-氨基己酸引入流化的氧化铝床中并在290°至400°的蒸气存在下进行处理 C。

公开(公告)号：US4518602A

公开(公告)日：1985-05-21

申请号：US537862

申请日：1983-09-30

Applicant: Shinji Terao ,  Kohei Nishikawa

Inventor： Shinji Terao ,  Kohei Nishikawa

IPC: C07C51/363 ,  C07D201/08 ,  C07D213/26 ,  C07D213/30 ,  C07D213/32 ,  C07D213/50 ,  C07D213/55 ,  C07D213/57 ,  C07D405/06 ,  C07D409/04 ,  C07D409/06 ,  C07F9/54 ,  A61K31/44 ,  C07D211/82 ,  C07D407/06

CPC classification number: C07D213/30 ,  C07C51/363 ,  C07D201/08 ,  C07D213/26 ,  C07D213/32 ,  C07D213/50 ,  C07D213/55 ,  C07D213/57 ,  C07D405/06 ,  C07D409/04 ,  C07D409/06 ,  C07F9/5407

Abstract: Novel compound of the formula: ##STR1##wherein R.sup.1 is a pyridyl group; R.sup.2 is a phenyl, thienyl, furyl, naphthyl, benzothienyl or pyridyl group which may have as a substituent a lower alkoxy, a lower alkyl, a halogen, trifluoromethyl, a lower alkenyl or methylenedioxy; R.sup.3 is hydrogen, benzyl or a lower alkyl; one of R.sup.4 and R.sup.5 is hydrogen or a lower alkyl, and the other is an aryloxy, or lower aliphatic hydrocarbon, an alicyclic hydrocarbon having not more than 6 carbon atoms or an aromatic group which may have a substituent, or a group represented by the formula, --S(O).sub.m --R.sup.6 (in which R.sup.6 is phenyl or a lower alkyl group; m is an integer of 0 to 2), or R.sup.4 and R.sup.5 each combine with the other to represent one alkylene group; n is an integer of 2 to 6, or a pharmaceutically acceptable salt thereof has a selective inhibitory action on bio-synthesis of thromboxane A.sub.2 (TXA.sub.2) and an effect of enhancing the production of prostaglandin I.sub.2 (PGI.sub.2), and can be used in mammals for to prevention and treatment of arterial thrombosis caused by platelet aggregation or ischemic diseases caused by vasospasms in cardiac, cerebral and peripheral circulatory system (e.g. cardian infarction, apoplexy, infarct of blood vessels in kidney, lung and other organs, pectic ulcer, etc.).

Abstract translation: 下式的新型化合物：其中R 1是吡啶基; R2是可以具有低级烷氧基，低级烷基，卤素，三氟甲基，低级烯基或亚甲二氧基的取代基的苯基，噻吩基，呋喃基，萘基，苯并噻吩基或吡啶基。 R3是氢，苄基或低级烷基; R4和R5中的一个是氢或低级烷基，另一个是芳氧基或低级脂族烃，不大于6个碳原子的脂环族烃或可以具有取代基的芳族基团，或由 式（-S（O）m -R 6（其中R 6为苯基或低级烷基; m为0〜2的整数），或者R 4和R 5各自与一个亚烷基结合， n为2〜6的整数，或其药学上可接受的盐对凝血恶烷A2（TXA2）的生物合成具有选择性抑制作用和增强前列腺素I2（PGI2）的产生的作用，可用于哺乳动物 用于预防和治疗由心脏，脑和周围循环系统（例如心脏梗塞，中风，肾脏，肺部和其他器官中的血管梗死，果胶性溃疡等）引起的血小板聚集或血管痉挛引起的缺血性疾病引起的动脉血栓形成。 ）。

公开(公告)号：US4470928A

公开(公告)日：1984-09-11

申请号：US420883

申请日：1982-09-21

Applicant: Kohji Kimura ,  Toshiro Isoya

Inventor： Kohji Kimura ,  Toshiro Isoya

IPC: C07D201/02 ,  C07D201/08 ,  C07D223/08 ,  C07D223/10 ,  C07C120/00 ,  C07C121/16 ,  C07C121/407

CPC classification number: C07C255/00 ,  C07D201/08 ,  Y02P20/52

Abstract: Caprolactam can be produced with an economical advantage without formation of by-products in a high yield by subjecting adipic acid and adiponitrile to interchange reaction at an elevated temperature, adding an alcohol directly to the interchange reaction mixture without isolating the resulting cyanovaleric acid to esterify the cyanovaleric acid with said alcohol into a cyanovaleric ester, reducing the cyanovaleric ester with a catalyst into an aminocaproic ester, heating the aminocaproic ester in a polyhydric alcohol having a higher boiling point than that of caprolactam to convert the ester into caprolactam, isolating the caprolactam by distillation and recycling the liquid distillation residue to the system for heating said polyhydric alcohol and said aminocaproic ester.

Abstract translation: 可以生产具有经济优势的己内酰胺，而不会通过使己二酸和己二腈在升高的温度下进行交换反应而以高产率形成副产物，直接向交换反应混合物中加入醇，而不分离得到的氰基戊酸酯化 将氰基戊酸与所述醇反应成氰基戊酸酯，用催化剂将氰基戊酸酯还原成氨基己酸酯，加热沸点高于己内酰胺的多元醇中的氨基己酸酯将酯转化为己内酰胺，将己内酰胺转化为己内酰胺 蒸馏并将液体蒸馏残余物再循环到用于加热所述多元醇和所述氨基己酸酯的体系中。